- BODIPY-based fluorescent probes for mitochondria-targeted cell imaging with superior brightness, low cytotoxicity and high photostability
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Two mitochondria-targeted fluorescent probes (TPP- and TEA-BODIPY) were rationally designed and easily synthesized. These probes can specifically stain mitochondria in living cells with superior brightness, low cytotoxicity and high photostability, thus a
- Gao, Tao,He, Huan,Huang, Rong,Zheng, Mai,Wang, Fang-Fang,Hu, Yan-Jun,Jiang, Feng-Lei,Liu, Yi
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- New BODIPYs for photodynamic therapy (PDT): Synthesis and activity on human cancer cell lines
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A new class of compounds based on the 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene core, known as BODIPYs, has attracted significant attention as photosensitizers suitable for application in photodynamic therapy (PDT), which is a minimally invasive procedur
- Caruso, Enrico,Malacarne, Miryam C.,Marras, Emanuela,Papa, Ester,Bertato, Linda,Banfi, Stefano,Gariboldi, Marzia B.
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- Efficient solution-processed deep-blue CIEy∈ (0.05) and pure-white CIEx,y∈ (0.34, 0.32) organic light-emitting diodes: experimental and theoretical investigation
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In this work, two bipolar non-conjugated deep-blue emitters, PICFOCz and BICFOCz, were synthesized by incorporating the charge transporting carbazole (donor/hole transporting) and imidazole (acceptor/electron-transporting) moietiesviaa flexible alkyl spac
- Tagare, Jairam,Yadav, Rohit Ashok Kumar,Swayamprabha, Sujith Sudheendran,Dubey, Deepak Kumar,Jou, Jwo-Huei,Vaidyanathan, Sivakumar
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- Targeted fluorescence lifetime probes reveal responsive organelle viscosity and membrane fluidity
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The only way to visually observe cellular viscosity, which can greatly influence biological reactions and has been linked to several human diseases, is through viscosity imaging. Imaging cellular viscosity has allowed the mapping of viscosity in cells, an
- Steinmark, Ida Emilie,James, Arjuna L.,Chung, Pei-Hua,Morton, Penny E.,Parsons, Maddy,Dreiss, Cécile A.,Lorenz, Christian D.,Yahioglu, Gokhan,Suhling, Klaus
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- Effect of carbazole functionalization with a spacer moiety in the phenanthroimidazole bipolar ligand in a europium(iii) complex on its luminescence properties: combined experimental and theoretical study
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The functionalization of carbazole with a spacer in the C1 position and fluorine in the N1 position in the imidazole phenanthroline based bipolar ligand has been designed, synthesised and utilized to make a Eu(TTA)3Phen-Fl-O-CBZ complex. The ab
- Rajamouli, Boddula,Sivakumar, Vaidyanthan
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- A bright, red-emitting water-soluble BODIPY fluorophore as an alternative to the commercial Mito Tracker Red for high-resolution mitochondrial imaging
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With the emergence and rapid development of super-resolution fluorescence microscopy, monitoring of mitochondrial morphological changes has aroused great interest for exploring the role of mitochondria in the process of cell metabolism. However, in the absence of water-soluble, photostable and low-toxicity fluorescent dyes, ultra-high-resolution mitochondrial imaging is still challenging. Herein, we designed two fluorescent BODIPY dyes, namelyMito-BDP 630andMito-BDP 760, for mitochondrial imaging. The results proved thatMito-BDP 760underwent aggregation-caused quenching (ACQ) in the aqueous matrix owing to its hydrophobicity and was inaccessible to the cells, which restricted its applications in mitochondrial imaging. In stark contrast, water-solubleMito-BDP 630readily penetrated cellular and mitochondrial membranes for mitochondrial imaging with high dye densities under wash-free conditions as driven by membrane potential. As a comparison, Mito Tracker Red presented high photobleaching (the fluorescence intensity dropped by nearly 50%) and high phototoxicity after irradiation by a laser for 30 min. However,Mito-BDP 630possessed excellent biocompatibility, photostability and chemical stability. Furthermore, clear and bright mitochondria distribution in living HeLa cells after incubation withMito-BDP 630could be observed by CLSM. Convincingly, the morphology and cristae of mitochondria could be visualized using an ultra-high-resolution microscope. In short,Mito-BDP 630provided a powerful and convenient tool for monitoring mitochondrial morphologies in living cells. Given the facile synthesis, photobleaching resistance and low phototoxicity ofMito-BDP 630, it is an alternative to the commercial Mito Tracker Red.
- Chen, Ji-Lei,Gao, Lian-Xun,Jiang, Feng-Lei,Liu, Yi,Wang, Jiang-Lin,Zhang, Lu,Zhou, Te
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supporting information
p. 8639 - 8645
(2021/11/04)
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- Chelidamic acid derivatives: Precursors to functionalized pyridyl cryptands & functionalized metal ligands
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Pyridyl cryptands, such as 12–16 formed from pyridine-2,6-dicarbonyl chloride (4) and crown ether diols 7–11, have been demonstrated to be excellent hosts for viologens (N,N′-dialkyl-4,4′-bipyridinium salts, 2) with Ka values of ~104
- Gibson, Harry W.,Nellipalli, Pothanagandhi,Niu, Zhenbin,Pederson, Adam M.-P.,Price, Terry L.
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- Design, synthesis and evaluation of novel dimethylamino chalcone-O-alkylamines derivatives as potential multifunctional agents against Alzheimer's disease
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A novel series of dimethylamino chalcone-O-alkylamines derivatives was designed and synthesized as multifunctional agents for the treatment of AD. All the target compounds exhibited significant abilities to inhibit and disaggregate Aβ aggregation, and acted as potential selective AChE inhibitors, biometal chelators and selective MAO-B inhibitors. Among these compounds, compound TM-6 showed the greatest inhibitory activity against self-induced Aβ aggregation (IC50 = 0.88 μM) and well disaggregation ability toward self-induced Aβ aggregation (95.1%, 25 μM), the TEM images, molecular docking study and molecular dynamics simulations provided reasonable explanation for its high efficiency, and it was also found to be a remarkable antioxidant (ORAC-FL values of 2.1eq.), the best AChE inhibitor (IC50 = 0.13 μM) and MAO-B inhibitor (IC50 = 1.0 μM), as well as a good neuroprotectant. UV–visual spectrometry and ThT fluorescence assay revealed that compound TM-6 was not only a good biometal chelator by inhibiting Cu2+-induced Aβ aggregation (95.3%, 25 μM) but also could disassemble the well-structured Aβ fibrils (88.1%, 25 μM). Further, TM-6 could cross the blood-brain barrier (BBB) in vitro. More importantly, compound TM-6 did not show any acute toxicity in mice at doses of up to 1000 mg/kg and improved scopolamine-induced memory impairment. Taken together, these data indicated that TM-6, an excellent balanced multifunctional inhibitor, was a potential lead compound for the treatment of AD.
- Sang, Zhipei,Song, Qing,Cao, Zhongcheng,Deng, Yong,Tan, Zhenghuai,Zhang, Li
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- Novel imidazole-alkyl spacer-carbazole based fluorophores for deep-blue organic light emitting diodes: Experimental and theoretical investigation
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A series of fluorescent emitters based on Imidazole-Alkyl spacer-Carbazole were designed and synthesized by connecting donor and acceptor moieties through alkyl spacer. In these design strategy we have chosen carbazole as electron rich and imidazole as electron deficient with deferent functional black (phenyl and phenyl substituted) at the N1 position of imidazole moiety. All the fluorophores were structurally confirmed by spectroscopic methods (NMR, MASS, and FTIR). The photophysical, electrochemical and electroluminescence properties were thoroughlyexamined. All the fluorophores showed good thermal stability and near-UV emission with high photoluminescence quantum yield (PLQY)of ~59% in the solid state. All the synthesized compounds feature Commission International de L'Eclairage (CIE) coordinates of y 0.08 for a particular doping concentration, which is very close to the National Television Standards Committee (NTSC) standard blue (0.14, 0.08). Solution-processed organic light emitting diode (OLED) device consisting of molecule BIPOCz displays a maximum external quantum efficiency EQE of 1.9% with CIE coordinates of (0.17, 0.07). All these results reveal that this work provides novel approaches for realizing ultra-deep-blue emission with high performance.
- Boddula, Rajamouli,Dubey, Deepak Kumar,Jou, Jwo-Huei,Patel, Sabita,Tagare, Jairam,Vaidyanathan, Sivakumar,Yadav, Rohit Ashok Kumar
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- Tailoring the Solid-State Fluorescence of BODIPY by Supramolecular Assembly with Polyoxometalates
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A cationic boron dipyrromethene (BODIPY) derivative (1+) has been successfully combined with two polyoxometalates (POMs), the Lindqvist-type [W6O19]2- and the β-[Mo8O26]4- units, into three new supramolecular fluorescent materials (1)2[W6O19]·2CH3CN, (1)2
- Bolle, Patricia,Benali, Tarik,Menet, Clotilde,Puget, Marin,Faulques, Eric,Marrot, Jér?me,Mialane, Pierre,Dolbecq, Anne,Serier-Brault, Hélène,Oms, Olivier,Dessapt, Rémi
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supporting information
p. 12602 - 12609
(2021/08/24)
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- Liquid crystal behavior, photoluminescence and gas sensing: A new series of ionic liquid crystal imidazole and benzoimidazole bearing chalcone groups, synthesis and characterization
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Four new series of chalcones containing imidazole bromonium and benzimidazole bromonium salts with spacer alkyl chains (Cn, n = 2 and 4) were synthesized and the chemical structure, thermal behavior, photoluminescence and gas sensing were characterized by
- Abbas, Wahaj Raed,Mohammad, Abdulkarim-Talaq
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p. 38444 - 38456
(2021/12/20)
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- Efficient near ultraviolet emissive (CIE: Y < 0.06) organic light-emitting diodes based on phenanthroimidazole-alkyl spacer-carbazole fluorophores: Experimental and theoretical investigation
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Efficient near ultraviolet light-emitting materials are of particular importance in organic light emitting devices (OLEDs) because of their potential for application in high-quality flat panel displays and white OLEDs. In the present investigation, a seri
- Tagare, Jairam,Boddula, Rajamouli,Sudheendran, Sujith Swayamprabha,Dubey, Deepak Kumar,Jou, Jwo-Huei,Patel, Sabita,Vaidyanathan, Sivakumar
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supporting information
p. 16834 - 16844
(2020/12/30)
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- Design, synthesis and biological evaluation of 2,3-dihydro-5,6-dimethoxy-1H-inden-1-one and piperazinium salt hybrid derivatives as hAChE and hBuChE enzyme inhibitors
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2,3-Dihydro-5,6-dimethoxy-2-[4-(4-alkyl-4-methylpiperazinium-1-yl)benzylidine]-1H-inden-1-one halide salt derivatives as a novel donepezil hybrid analogs with the property of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzyme inhibition were designed and synthesized via N-alkylation reaction of 2,3-dihydro-5,6-dimethoxy-2-[4-(4-methylpiperazin-1-yl)benzylidene]-1H-inden-1-one with some alkyl halides. Biological tests demonstrated that most of the synthesized compounds have moderate to good inhibitory activities effect on cholinesterase enzymes. Among them, 10e showed the best profile as a selected compound for inhibition of hAChE (IC50 = 0.32) and hBuChE (IC50 = 0.43 μM) enzymes. Kinetic analysis and molecular docking led to a better understanding of this compound. Kinetic studies disclosed that 10e inhibited acetylcholinesterase in mixed-type and butyrylcholinesterase in non-competitive type. The toxicity results showed that 10e is less toxic than donepezil and has better inhibitory activity against hBuChE when compared to donepezil or Galantamine. Other performed experiments revealed that 10e has an anti-β amyloid effect which is capable of reducing ROS, LDH and MDA also possing positive effect on TAC. On the other hand, it has shown a good anti-inflammation effect.
- Mozaffarnia, Sakineh,Rashidi, Mohammad-Reza,Teimuri-Mofrad, Reza
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- A novel water-soluble BODIPY dye as red fluorescent probe for imaging hypoxic status of human cancer cells
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The development of effective methods for real-time monitoring of nitroreductase (NTR) activity is of great significance for medical diagnosis and cancer research. Here, we present a novel water-soluble BODIPY-based chemodosimeter (NBB) for imaging the hypoxic status of human non-small-cell lung cancer A549 cells. We assume that ‘on–off’ response of NBB is activated by the NTRmediated reductive release of meso-phenol BODIPY dye resulting in unusual fluorescence.
- Gorbatov, Sergey A.,Romieu, Anthony,Scherbakov, Alexander M.,Uvarov, Denis Yu.,Volkova, Yulia A.,Zavarzin, Igor V.
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p. 750 - 752
(2021/01/11)
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- The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease
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In this work, we have developed a novel series of multi-target-directed ligands to address low levels of acetylcholine (ACh), oxidative stress, metal ion dysregulation, and the misfolded proteins. Novel apigenin-donepezil derivatives, naringenin-donepezil derivatives, genistein-donepezil derivatives and chalcone-donepezil derivatives have been synthesized, in vitro results showed that TM-4 was a reversible and potent huAChE (IC50 = 0.36 μM) and huBChE (IC50 = 15.3 μM) inhibitor, and showed potent antioxidant activity (ORAC = 1.2 eq). TM-4 could significantly inhibit self-induced Aβ1-42 aggregation (IC50 = 3.7 μM). TM-4 was also an ideal neuroprotectant, potential metal chelation agent, and it could inhibit and disaggregate huAChE-induced and Cu2+-induced Aβ aggregation. Moreover, TM-4 could activate UPS degradation pathway in HT22 cells and induce autophagy on U87 cells to clear abnormal proteins associated with AD. More importantly, TM-4 could cross BBB in vitro assay. In addition, in vivo assay revealed that TM-4 exhibited remarkable dyskinesia recovery rate and response efficiency on AlCl3-induced zebrafish AD model, and TM-4 indicated surprising protective effect on Aβ1-40-induced vascular injury. TM-4 presented precognitive effect on scopolamine-induced memory impairment. And the regulation of multi-targets for TM-4 were further conformed through transcriptome sequencing. More interesting, the blood, urine and feces metabolism in rat and rat/human liver microsome metabolism towards TM-4 were also investigated. Overall, TM-4 is a promising multi-function candidate for the development of drugs to Alzheimer's disease.
- Cheng, Xinfeng,Liu, Wenmin,Qiao, Zhanpin,Sang, Zhipei,Shi, Jian,Tan, Zhenghuai,Wang, Keren,Wang, Yiling,Wu, Anguo,Zhao, Yiyang,Zhu, Gaofeng
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- Nickel-Catalyzed Multicomponent Coupling Reaction of Alkyl Halides, Isocyanides and H2O: An Expedient Way to Access Alkyl Amides
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We herein describe a Ni-catalyzed multicomponent coupling reaction of alkyl halides, isocyanides, and H2O to access alkyl amides. Bench-stable NiCl2(dppp) is competent to initiate this transformation under mild reaction conditions, thus allowing easy operation and adding practical value. Substrate scope studies revealed a broad functional group tolerance and generality of primary and secondary alkyl halides in this protocol. A plausible catalytic cycle via a SET process is proposed based on preliminary experiments and previous literature.
- Li, Qiao,Jin, Hongwei,Liu, Yunkui,Zhou, Bingwei
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supporting information
p. 3466 - 3472
(2020/09/15)
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- A dual-acting 5-HT6 receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties
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The complex etiology of Alzheimer's disease has initiated a quest for multi-target ligands to address the multifactorial causes of this neurodegenerative disorder. In this context, we designed dual-acting 5-HT6 receptor (5-HT6R) anta
- Canale, Vittorio,Grychowska, Katarzyna,Kurczab, Rafa?,Ryng, Mateusz,Keeri, Abdul Raheem,Sata?a, Grzegorz,Olejarz-Maciej, Agnieszka,Koczurkiewicz, Paulina,Drop, Marcin,Blicharz, Klaudia,Piska, Kamil,P?kala, El?bieta,Janiszewska, Paulina,Krawczyk, Martyna,Walczak, Maria,Chaumont-Dubel, Severine,Bojarski, Andrzej J.,Marin, Philippe,Popik, Piotr,Zajdel, Pawe?
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supporting information
(2020/09/21)
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- Synthesis and photodynamic activity of novel non-symmetrical diaryl porphyrins against cancer cell lines
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Photodynamic therapy (PDT)of cancer uses photosensitizers (PS), a light source and oxygen to generate high levels of reactive oxygen species (ROS), that exert a cytotoxic action on tumor cells. Recently, it has been shown that mixed non-symmetrical diaryl porphyrins, with two different pendants, are more photodynamically active than symmetrical diaryl porphyrins. In the present study, we investigate the in vitro photodynamic effects of four novel non-symmetrical diaryl porphyrins, two of which bear one pentafluoro-phenyl and one bromo-alkyl (apolar)pendant, whereas the two others bear one pentafluoro-phenyl and one cationic pyridine pendant. The four compounds were tested in a small panel of human cancer cell lines, and their photodynamic activities were compared with that of m-THPC (Foscan), currently the most successful PS approved for clinical use in cancer PDT. The results of the cytotoxicity studies indicate that the two molecules bearing the cationic pendant are more potent in vitro than those with the apolar pendant, and that they are as potent as Foscan. To gain further insights into the mechanism of PS-induced phototoxicity, induction of apoptotic, autophagic and necrotic cell death, and generation of reactive oxygen species (ROS)were evaluated in cancer cells following exposure to the PSs and irradiation. The effect of the PSs on the migratory activity of the cells was also assessed. The data obtained from this work support a greater potency of diaryl porphyrins with a positive charge in inducing cell death, as compared to those with the bromo-alkyl pendant; most importantly, some of these novel compounds exhibit features that might make them superior to the clinically approved PS Foscan.
- Caruso, Enrico,Cerbara, Monica,Malacarne, Miryam Chiara,Marras, Emanuela,Monti, Elena,Gariboldi, Marzia Bruna
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- Preparation of aggregation-induced emission material with light stability
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The invention discloses a hindered amine light stabilizer with an aggregation-induced emission (AIE) performance and a synthesis method thereof. The hindered amine light stabilizer is formed through steps including a step of ensuring that AIE pyrone deriv
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Paragraph 0040; 0041
(2019/02/27)
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- Hydrazide–Hydrazone Small Molecules as AIEgens: Illuminating Mitochondria in Cancer Cells
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Aggregation-induced-emission luminogens (AIEgens) have gained considerable attention as interesting tools for several biomedical applications, especially for bioimaging due to their brightness and photostability. Numerous AIEgens have been developed for lighting up the subcellular organelles to understand their forms and functions not only healthy but also unhealthy states, such as in cancer cells. However, there is lack of easily synthesizable, biocompatible small molecules for illuminating mitochondria (powerhouses) inside cells. To address this issue, an easy and short synthesis of new biocompatible hydrazide–hydrazone-based small molecules with remarkable aggregation-induced emission (AIE) properties is described. These small-molecule AIEgens showed hitherto unobserved AIE properties due to dual intramolecular H-bonding confirmed by theoretical calculation, pH- and temperature-dependent fluorescence and X-ray crystallographic studies. Confocal microscopy showed that these AIEgens were internalized into the HeLa cervical cancer cells without showing any cytotoxicity. One of the AIEgens was tagged with a triphenylphosphine (TPP) moiety, which successfully localized in the mitochondria of HeLa cells in a selective way compared to L929 noncancerous fibroblast cells. These unique hydrazide–hydrazone-based biocompatible AIEgens can serve as powerful tools to illuminate multiple subcellular organelles to elucidate their forms and functions in cancer cells for next-generation biomedical applications.
- Patil, Sohan,Pandey, Shalini,Singh, Amit,Radhakrishna, Mithun,Basu, Sudipta
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supporting information
p. 8229 - 8235
(2019/05/28)
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- Synthesis and evaluation of the in vitro antimicrobial activity of triazoles, morpholines and thiosemicarbazones
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Background: Microbial infections is a global public health problem. The aim of this work was to synthesize and evaluate the antimicrobial activity of novel triazoles, morpholines and thiosemicarbazones. Methods: Compounds were synthesized using 2,4-Dihydroxyacetophenone and 4-hydroxybenzaldehyde as starting materials. The antimicrobial activity of these compounds against bacteria and yeast was evaluated by the broth microdilution method. Results: The proposed route for synthesis gave high to moderate yields, moreover these compounds were successfully characterized by 1H NMR, 13C NMR and LC-MS. Antimicrobial testing indicated that the thiosemicarbazone and morphine derivatives had the best antimicrobial activity against the microorganisms tested with minimum inhibitory concentrations (MIC) between 0.29 and 5.30 μM. Thiosemicarbazone derivative (12) was able to inhibit the growth of C. tropicalis, with minimum fungicidal concentration (MFC) of 0.55 μM. In addition, this compound was active against E. coli, S. aureus and S. epidermidis, with MIC values ranging from 0.29 to 1.11 μM. Moreover, the morpholine derivative (15) had an MIC value of 0.83 μM against C. albicans and E. coli. Conclusion: We have efficiently synthesized a series of eleven novel triazoles, thiosemicarbazones and morpholine derivatives using 2,4-Dihydroxyacetophenone and 4-hydroxybenzaldehyde as starting materials. Thiosemicarbazone derivative (12) showed promising antifungal and antibacterial activity and these findings suggest that this compound can be used as scaffolds to design new antimicrobial drugs.
- Andradeb, Jéssica T.,Araújoc, Marcelo G. F.,Carmo, Lucas F.,Fernandesa, Joice S.,Ferreirab, Jaqueline M. S.,Santosa, Felipe R. S.,Sousab, Carla D. F.,Villar, José A. F. P.
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- Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease
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A series of novel chalcone-O-alkylamine derivatives were designed, synthesized and evaluated as multifunctional anti-Alzheimer's disease agents. Based on the experimental results, compound 23c exhibited good inhibitory potency on both acetylcholinesterase
- Bai, Ping,Wang, Keren,Zhang, Pengfei,Shi, Jian,Cheng, Xinfeng,Zhang, Qi,Zheng, Cheng,Cheng, Yao,Yang, Jian,Lu, Xiaoxia,Sang, Zhipei
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- FLUORENE-BASED COMPOUND, ORGANIC LIGHT EMITTING DEVICE USING THE SAME AND METHOD OF MANUFACTURING THE SAME
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The present invention relates to a fluorine-based compound of chemical formula 1, a coating composition including the fluorine-based compound of chemical formula 1, an organic light emitting device using the same, and a manufacturing method thereof. In chemical formula 1, L1 and L2 are identical or different and is independently a substituted or unsubstituted alkylene group; a substituted or unsubstituted cycloalkylene group; or a substituted or unsubstituted hetero arylene group; and L is a substituted or unsubstituted arylene group, or a substituted or unsubstituted heteroarylene group.COPYRIGHT KIPO 2018
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Paragraph 0303-0306
(2018/10/03)
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- Mitochondria target fluorescence probe, as well as preparation method and application thereof
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The invention discloses a mitochondria target fluorescence probe, as well as a preparation method and application thereof. The probe has a structure as shown in formula (I). The mitochondria target fluorescence probe can overcome the defects of the tradit
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Paragraph 0023; 0033
(2017/04/03)
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- Synthesis of new α-aminophosphonate derivatives incorporating benzimidazole, theophylline and adenine nucleobases using l-cysteine functionalized magnetic nanoparticles (LCMNP) as magnetic reusable catalyst: Evaluation of their anticancer properties
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A new class of structurally diverse α-aminophosphonate derivatives containing benzimidazole, theophylline and adenine heterocycles were synthesized using a simple and efficient strategy. This class of α-aminophosphonates was synthesized using the reaction
- Bahrami, Foroogh,Panahi, Farhad,Daneshgar, Fatemeh,Yousefi, Reza,Shahsavani, Mohammad Bagher,Khalafi-Nezhad, Ali
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p. 5915 - 5924
(2016/02/05)
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- Hybrid pharmacophore design and synthesis of naphthalimide-benzimidazole conjugates as potential anticancer agents
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Naphthalimide-benzimidazole conjugates were prepared using two different types of spacer units; either a simple alkane chain or a substituted piperazine moiety with variable alkyl side chains. Each set of conjugates was evaluated for their in vitro antica
- Kamal, Ahmed,Kumar, Pogula Praveen,Khan, Mohammed Naseer Ahmed,Sheshadri, Bobburi Naga,Srinivas, Olepu
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p. 374 - 384
(2015/06/22)
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- Multitarget-directed resveratrol derivatives: Anti-cholinesterases, anti-β-amyloid aggregation and monoamine oxidase inhibition properties against Alzheimer's disease
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Considering the complex pathogenesis factors of Alzheimer's disease (AD), the multitarget-directed ligand strategy is expected to provide superior effects to fight AD, instead of the classic one-drug-one-target strategy. Resveratrol, exhibiting important properties against AD, was suggested to be used as a starting compound for the treatment of AD. Based on these reasons, a series of resveratrol derivatives were designed, synthesized and biologically evaluated. Among them, compound 6r, exhibiting moderate cholinesterase inhibition activity (AChE, IC50 = 6.55 μM; BuChE, IC50 = 8.04 μM; SI = 1.23), significant inhibition of Aβ42 aggregation (57.78%, at 20 μM) and acceptable inhibitory activity against monoamine oxidases (MAO-A, IC50 = 17.58 μM; MAO-B, IC50 = 12.19 μM), was a potential anti-Alzheimer agent with balanced activities. Consequently, this study provided useful information for further development of resveratrol derivatives as multitarget-directed agents for AD therapy. This journal is the Partner Organisations 2014.
- Pan, Long-Fei,Wang, Xiao-Bing,Xie, Sai-Sai,Li, Su-Yi,Kong, Ling-Yi
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supporting information
p. 609 - 616
(2014/05/06)
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- NSAIDs DERIVATIVES AND USES THEREOF
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The present invention discloses novel compounds derived from NSAIDs and pharmaceutically acceptable salts thereof. Other aspects of the invention relate to use of the NSAID derivatives in treating inflammatory diseases and pharmaceutical compositions ther
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Page/Page column 34-35
(2014/08/20)
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- Synthesis and characterization of 1H-phenanthro[9,10-d]imidazole derivatives as multifunctional agents for treatment of Alzheimer's disease
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Background Alzheimer's disease (AD) is a progressive neurodegenerative brain disorder that is characterized by dementia, cognitive impairment, and memory loss. Diverse factors are related to the development of AD, such as increased level of β-amyloid (Aβ), acetylcholine, metal ion deregulation, hyperphosphorylated tau protein, and oxidative stress. Methods The following methods were used: organic syntheses of 1H-phenanthro[9,10-d] imidazole derivatives, inhibition of self-mediated and metal-induced Aβ1-42 aggregation, inhibition studies for acetylcholinesterase and butyrylcholinesterase, anti-oxidation activity studies, CD, MTT assay, transmission electron microscopy, dot plot assay, gel electrophoresis, Western blot, and molecular docking studies. Results We synthesized and characterized a new type of 1H-phenanthro[9,10-d]imidazole derivatives as multifunctional agents for AD treatment. Our results showed that most of these derivatives exhibited strong Aβ aggregation inhibitory activity. Compound 9g had 74% Aβ1-42 aggregation inhibitory effect at 10 μM concentration with its IC50 value of 6.5 μM for self-induced Aβ1-42 aggregation. This compound also showed good inhibition of metal-mediated (Cu2 + and Fe2 +) and acetylcholinesterase-induced Aβ1-42 aggregation, as indicated by using thioflavin T assay, transmission electron microscopy, gel electrophoresis, and Western blot. Besides, compound 9g exhibited cholinesterase inhibitory activity, with its IC50 values of 0.86 μM and 0.51 μM for acetylcholinesterase and butyrylcholinesterase, respectively. In addition, compound 9g showed good anti-oxidation effect with oxygen radical absorbance capacity (ORAC) value of 2.29. Conclusions Compound 9g was found to be a potent multi-target-directed agent for Alzheimer's disease. General significance Compound 9g could become a lead compound for further development as a multi-target-directed agent for AD treatment.
- Liu, Jinggong,Qiu, Jun,Wang, Mingxue,Wang, Ling,Su, Lijuan,Gao, Jinbo,Gu, Qiong,Xu, Jun,Huang, Shi-Liang,Gu, Lian-Quan,Huang, Zhi-Shu,Li, Ding
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p. 2886 - 2903
(2014/07/21)
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- Hyperbranched polyethers with tunable glass transition temperature: Controlled synthesis and mixing rules
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By taking advantage of competing side reactions, controlled synthesis of a series of homo- and co-polymerized hyperbranched polyethers (HBPEs) is demonstrated using AB2 monomers of different spacer lengths. This reacting system shows good controllability and scalability. More importantly, the degree of branching is found to be insensitive to the molecular weight and spacer length in monomers. Thus, the value and width of Tg can be tuned by varying monomer spacer length, terminal groups, molecular weight, as well as by copolymerization and physical blending. The dependence of T g in binary homopolymer blends on composition and the dependence of Tg in copolymers on monomer ratio are established and compared for the first time. Tg of copolymers obeys the Fox equation, whereas Tg in binary blends only follows the Kwei equation. Copolymerization does not increase the width of Tg. In contrast, the width of T g of binary blends is much broader than that of copolymers, even though the broadening in Tg can be reduced by increasing the polarity of terminal groups. the Partner Organisations 2014.
- Liu, Tuan,Geng, Xinxin,Nie, Yongxing,Chen, Ruoshi,Meng, Yan,Li, Xiaoyu
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p. 30250 - 30258
(2014/08/05)
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- Synthesis of novel dithiocarbamyl-containing organosilicon compounds
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Aldehydes-bearing dithiocarbamate moieties were generated via highly efficient and simple method based on the one-pot reaction of amines, CS2, and 4-(bromoalkoxy)benzaldehydes with the use of K2CO3 as a catalyst under solv
- Safa, Kazem D.,Tavakkoli Osgoei, Sama,Alyari, Maryam
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p. 683 - 690
(2015/10/19)
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- Synthesis of thiophene and NO-curcuminoids for antiinflammatory and anti-cancer activities
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In search of better NSAIDs four novel nitric oxide donating derivatives of curcumin (compounds 9a-d), and four thiophene curcuminoids (compounds 10a-c, 11) have been synthesised. The cytotoxic effects of these compounds along with the lead compound curcumin (7) and their effect on the production of the reactive oxygen species nitric oxide and pro-inflammatory cytokines IL-1β, TNF-α and chemokine CXCL-8 were evaluated using human monocytic THP-1 and colon adenocarcinoma CACO-2 cell lines. All of the nitric oxide donating curcuminoids 9a-d and the thiophene curcuminoids 10a-c and 11 were non-cytotoxic to THP-1 cells over a concentration range of 10-100 μM and compared with curcumin compounds 10b and 10c, were more toxic. In CACO-2 cells, 10b and 11 appeared to be non-toxic at 10 to 50 μM, whereas 10a and 10c were non-cytotoxic at 10 μM only. These results clearly indicate that the introduction of a nitroxybutyl moiety to curcumin and replacement of phenyl rings with thiophene units reduces the cytotoxic effect of the parent curcumin, whereas a methyl substituted thiophene increases the cytotoxic effects. In THP-1 cells, drugs 10a and 11 significantly decreased IL-1-β production at their non-cytotoxic concentrations, whereas, they did not decrease TNF-α production in CACO-2 cells. Compound 11 showed a significant decrease in CXCL-8 production.
- Ahmed, Mahera M.,Khan, M. Akram,Rainsford, Kim Drummond
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p. 1483 - 1501
(2013/04/23)
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- Synthesis, antimalarial activity and cytotoxic potential of new monocarbonyl analogues of curcumin
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A series of novel monocarbonyl analogues of curcumin have been designed, synthesized and tested for their activity against Molt4, HeLa, PC3, DU145 and KB cancer cell lines. Six of the analogues showed potent cytotoxicity towards these cell lines with IC50 values below 1 μM, which is better than doxorubicin, a US FDA approved drug. Several analogues were also found to be active against both CQ-resistant (W2 clone) and CQ-sensitive (D6) strains of Plasmodium falciparum in an in-vitro antimalarial screening. This level of activity warrants further investigation of the compounds for development as anticancer and antimalarial agents.
- Manohar, Sunny,Khan, Shabana I.,Kandi, Shamseer Kulangara,Raj, Kranthi,Sun, Guojing,Yang, Xiaochuan,Calderon Molina, Angie D.,Ni, Nanting,Wang, Binghe,Rawat, Diwan S.
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supporting information
p. 112 - 116
(2013/02/23)
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- Synthesis and biological evaluation of nitric oxide releasing derivatives of 6-amino-3-n-butylphthalide as potential antiplatelet agents
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A series of novel nitric oxide releasing derivatives of 6-amino-3-n-butylphthalide were designed, synthesized and evaluated as potential antiplatelet agents. Compound 10b significantly inhibited the adenosine diphosphate (ADP)-induced platelet aggregation
- Wang, Xiaoli,Wang, Linna,Huang, Zhangjian,Sheng, Xiao,Li, Tingting,Ji, Hui,Xu, Jinyi,Zhang, Yihua
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p. 1985 - 1988
(2013/05/09)
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- Electrochemical and magnetic properties of a surface-grafted novel endohedral metallofullerene derivative
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A novel endohedral metallofullerene (EMF) has been designed and synthesised for its grafting on gold. The functionalization of the substrate resulted in a multifunctional surface displaying the properties of the EMF in solution.
- Crivillers, Nuria,Takano, Yuta,Matsumoto, Yuya,Casado-Montenegro, Javier,Mas-Torrent, Marta,Rovira, Concepcio,Akasaka, Takeshi,Veciana, Jaume
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supporting information
p. 8145 - 8147
(2013/09/12)
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- Tricolor emission of a fluorescent heteroditopic ligand over a concentration gradient of zinc(II) ions
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The internal charge transfer (ICT) type fluoroionophore arylvinyl-bipy (bipy = 2,2′-bipyridyl) is covalently tethered to the spirolactam form of rhodamine to afford fluorescent heteroditopic ligand 4. Compound 4 can be excited in the visible region, the e
- Sreenath, Kesavapillai,Clark, Ronald J.,Zhu, Lei
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p. 8268 - 8279
(2013/01/15)
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- 1,4-naphthoquinone cations as antiplasmodial agents: Hydroxy-, acyloxy-, and alkoxy-substituted analogues
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Cations of hydroxy-substituted 1,4-naphthoquinones were synthesized and evaluated as antiplasmodial agents against Plasmodium falciparum. The atovaquone analogues were found to be inactive as antagonists of parasite growth, which was attributed to ionization of the acidic hydroxyl moiety. Upon modification to an alkoxy substituent, the antiplasmodial activity was restored in the sub-100 nM range. Optimal inhibitors were found to possess IC50 values of 17.4-49.5 nM against heteroresistant P. falciparum W2.
- Lu, Xiao,Altharawi, Ali,Gut, Jiri,Rosenthal, Philip J.,Long, Timothy E.
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supporting information
p. 1029 - 1033
(2013/02/22)
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- Synthesis of photoactive bichromophoric dyads containing 2-styrylquinoline and 2-naphthol moieties
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A three-step approach to the synthesis of bichromophoric dyads of the general formula SQ - (CH2)n - Np (SQ is the 2-(4-oxystyryl)quinoline moiety, Np is the 3-oxy-2-naphthol moiety, n = 2, 4, 5) was developed from available reagents.
- Gavrishova,Li,Sadykova,Budyka
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experimental part
p. 1495 - 1499
(2012/07/13)
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- Synthesis of 4-[(diethylamino)methyl]-phenol derivatives as novel cholinesterase inhibitors with selectivity towards butyrylcholinesterase
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A series of novel cholinesterase inhibitors, being composed of 4-[(diethylamino)methyl]-phenoxy and secondary amine which were linked with a different length alkyl chain, were designed and synthesized from the starting material p-hydroxybenzaldehyde. Thes
- Yu, Liang,Cao, Rihui,Yi, Wei,Yan, Qin,Chen, Zhiyong,Ma, Lin,Peng, Wenlie,Song, Huacan
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experimental part
p. 3254 - 3258
(2010/09/04)
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- New 1,3-dioxolane and 1,3-dioxane derivatives as effective modulators to overcome multidrug resistance
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Multidrug resistance (MDR) to antitumor agents represents a major obstacle to a successful chemotherapy of cancer. Overexpression of P-glycoprotein (p-gp) seems to be the major factor responsible for MDR. A large number of chemically unrelated compounds are known to interact with p-gp resulting in a decreasing resistance. In our efforts related to structure-activity studies of new potential MDR reversal agents we synthesized a series of compounds that differ in the aromatic core structure, the linker, and the basic moiety. For our search of new aromatic core structures we synthesized novel 2,2-diphenyl-1,3-dioxolane, 2,2- diphenyl-1,3-dioxane, and 4,5-diphenyl-1,3-dioxolane derivatives. A range of lipophilic linker structures and protonable basic moieties were synthesized and investigated to optimize the structure of the potential MDR-modulators. The compounds were tested in vitro using human Caco-2 cells. Both the cytotoxicity of the synthons and their ability to resensitize the cells were determined with a MTT assay. The results show that at low concentration various substances reverse tumor cell MDR. Some of the new structures show better effects than established modulators like trifluoperazine.
- Schmidt, Matthias,Ungvari, Johannes,Gloede, Julia,Dobner, Bodo,Langner, Andreas
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p. 2283 - 2297
(2007/10/03)
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- Nanostructured oligo(p-phenylene vinylene)/silicate hybrid films: One-step fabrication and energy transfer studies
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Novel hybrid materials containing silicate and charged oligo(p-phenylene vinylene) (OPV) amphiphiles were fabricated in one step by spin casting using evaporation-induced self assembly. The conjugated segments were substituted with trimethylammonium bromide groups at both termini, and tetraethyl orthosilicate served as the silicate precursor. X-ray diffraction scans of the hybrid films revealed Bragg diffraction peaks with d-spacings of 2.76 and 1.37 nm, indicating the presence of order in the hybrid structure. Optical properties of the hybrid films were characterized by UV-vis absorption and fluorescence spectra, and molecular orientation was characterized by IR spectroscopy. A rhodamine B derivative containing a triethoxysilane group was covalently incorporated into the silicate network of the films during the sol-gel reaction. Relative to disordered polymer films with identical organic composition, the ordered hybrid films revealed significantly enhanced emission from rhodamine B and also fluorescence quenching from OPV segments. These results indicate that the ordered and nanostructured environment leads to highly efficient energy transfer among organic components in these hybrid films.
- Tajima, Keisuke,Li, Liang-Shi,Stupp, Samuel I.
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p. 5488 - 5495
(2007/10/03)
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- Formation of Stable Bilayer Assemblies in Dilute Aqueous Solution from Ammonium Amphiphiles with the Diphenylazomethine Segment
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Quarternary ammonium amphiphiles of the following structures were synthesized: Cn-BB-N+3C1 and Cn-BB-Cm-N+3C1, where Cn and Cm are hydrocarbon chains of n =
- Kunitake, Toyoki,Okahata, Yoshio
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p. 549 - 553
(2007/10/02)
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