- Liquid crystalline epoxy thermosets
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Rigid rod epoxy compounds can be cured in liquid crystalline structure. The so obtained networks exhibit better mechanical properties with respect to the isotropic ones. The mesogenic character of the epoxy compounds appears more crucial than the molecular geometry of the curing agent in developing liquid crystallinity. The curing temperature plays an important role in affecting the state of order of the thermosets.
- Giamberini,Amendola,Carfagna
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Read Online
- Antibacterial and anti-inflammatory activity of valproic acid-pyrazole conjugates as a potential agent against periodontitis
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Periodontitis is a serious global concern. Therefore, in the present study, we intend to synthesize novel valproic-acid pyrazole conjugates as a novel agent against periodontitis. The molecules were developed in a facile synthetic route and obtained in ex
- Dai, Xinxiang,Dong, Lei,Fang, Ling,Wang, Jia,Xu, Pei,Zhang, Jia
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Read Online
- 4,4'-DIHYDROXYCHALCONE FROM THE HEARTWOOD OF CHAMAECYPARIS OBTUSA
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A new chalcone, 4,4'-dihydroxychalcone was isolated from the heartwood of Chamaecyparis obtusa.The structure was elucidated by direct comparison with a synthetic sample.
- Ohashi, Hideo,Ido, Yoshimi,Imai, Takanori,Yoshida, Kazumasa,Yasue, Moritami
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Read Online
- Photo-sensitive benzoxazine II: Chalcone-containing benzoxazine and its photo and thermal-cured thermoset
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A chalcone-containing benzoxazine (BHP-a) was synthesized from a chalcone-containing bisphenol: 1,3-bis(4-hydroxyphenyl) propanone (BHP), aniline and paraformaldehyde in a co-solvent of xylene/1-butanol (2/1, V/V). The structure of BHP-a was successfully
- Lin, Ching Hsuan,Chien, Chun Kai,Chen, Chien Han,Juang, Tzong Yuan
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Read Online
- A simple and highly efficient method for the synthesis of chalcones by using borontrifluoride-etherate
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Chalcones are secondary metabolites of terrestrial plants, precursors for the biosynthesis of flavonoids and exhibit various biological activities. Condensation of substituted acetophenones (2a-12a) with various aromatic aldehydes (1b-7b) in the presence of BF3-Et2O at room temperature gave chalcones in 75-96% yield.
- Narender,Papi Reddy
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Read Online
- Method for efficiently synthesizing 1, 3-bis (4-hydroxyphenyl)-2-propylene-1-ketone
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The invention discloses a method for efficiently synthesizing 1, 3-bis (4-hydroxyphenyl)-2-propene-1-ketone, and belongs to the field of organic chemical synthesis. According to the method, a Claisen-Schmidt reaction is carried out, p-hydroxybenzaldehyde
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Paragraph 0024-0031
(2021/01/29)
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- Discovery of isoliquiritigenin analogues that reverse acute hepatitis by inhibiting macrophage polarization
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Screening a natural product library of 850 compounds yield isoliquiritigenin as an effective anti-inflammatory agent by inhibiting the production of pro-inflammatory NO induced by Pam3CSK4, while its activity accompanied by toxicity. Further studies obtained the optimized isoliquiritigenin derivative SMU-B14, which can inhibit Pam3CSK4 triggered toll-like receptor 2 (TLR2) signaling with low toxicity and high potency. Preliminary mechanism studies indicated that SMU-B14 worked through TLR2/MyD88, phosphorylation of IKKα/β, leading to the reduce degradation of NF-κB related IKBα and p65 complex, then inhibited the production of inflammatory cytokines, such as TNF-α, IL-6, IL-1β both in human and murine cell lines. Subsequent polarization experiments showed SMU-B14 significant reversed the polarization of M1 phenotype primary macrophage activated by Pam3CSK4 in vitro, and reduced the infiltration of neutrophil and polarization of M1-type macrophage, decreased serum alanine transaminase (ALT), as a result protected liver from being injured in vivo. In summary, we obtained an optimized lead compound SMU-B14 and found it functionally blocked TLR2/MyD88/NF-κB signaling pathway to down-regulate the production of inflammatory cytokines resulted significant liver protection property.
- Yang, Junjie,Hu, Fanjie,Guo, Chengjun,Liang, Yuqing,Song, Haiying,Cheng, Kui
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- Biocatalytic green alternative to existing hazardous reaction media: Synthesis of chalcone and flavone derivatives via the Claisen-Schmidt reaction at room temperature
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Owing to the increasing amount of waste materials around the globe, the conversion of waste or secondary by-products to value-added products for various applications has gained significant interest. Herein, two novel agro-food waste products, Musa sp. 'Malbhog' peel ash (MMPA) and Musa Champa Hort. ex Hook. F. peel ash (MCPA) are used as catalysts to promote an inexpensive, efficient and eco-friendly carbon-carbon bond forming crossed aldol reaction at room temperature in solvent free conditions. Furthermore, the resulting products were subjected to reactions with these promoters in an oxygen atmosphere and led to the formation of novel flavone derivatives. Moreover, the used catalysts were properly characterized using different sophisticated analytical techniques such as Fourier-transform infrared spectroscopy (FT-IR), X-ray diffractometry (XRD), Brunauer-Emmett-Teller analysis (BET), Raman spectroscopy, scanning electron microscopy energy dispersive X-ray spectroscopy (SEM-EDS), transition electron microscopy (TEM), X-ray photoelectron spectroscopy (XPS) and thermogravimetric analysis (TGA) along with element detection using atomic absorption spectroscopy and ion chromatographic methods. These two approaches are metal free, as well as being devoid of any extra additives, co-catalysts, harsh conditions, the use of column chromatography for purification and result in a higher yield of the product within a short space of time. The catalytic abilities of the promoter were also examined to synthesize important bioactive molecules such as butein and apigenin at room temperature. With gram scale synthesis of the chalcone derivatives, the used catalysts (MMPA and MCPA) were further reused for five cycles and did not demonstrate any loss in catalytic activity.
- Tamuli, Kashyap J.,Sahoo, Ranjan K.,Bordoloi, Manobjyoti
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supporting information
p. 20956 - 20965
(2020/12/31)
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- Chalcones and Chalcone-mimetic Derivatives as Notch Inhibitors in a Model of T-cell Acute Lymphoblastic Leukemia
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Based on hit-likeness and chemical diversity, a number of chalcones and chalcone-mimetic compounds were selected as putative Notch inhibitors. The evaluation of the antiproliferative effect combined with the inhibition of Notch1 expression in KOPTK1 cell line identified compound 18, featuring a tetrahydronaphthalene-based scaffold, as a new promising Notch-blocking agent.
- Quaglio, Deborah,Zhdanovskaya, Nadezda,Tobajas, Gloria,Cuartas, Viviana,Balducci, Silvia,Christodoulou, Michael S.,Fabrizi, Giancarlo,Gargantilla, Marta,Priego, Eva-María,Carmona Pestania, álvaro,Passarella, Daniele,Screpanti, Isabella,Botta, Bruno,Palermo, Rocco,Mori, Mattia,Ghirga, Francesca,Pérez-Pérez, María-Jesús
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supporting information
p. 639 - 643
(2019/04/25)
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- Crosslinking Monomers With at Least One Sulfur Atom
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The invention relates to a cross-linking monomer with at least one sulfur atom, representable by a structure of formula (I) wherein the symbols have the following meaning: L1 is a linear, branched or cyclic, saturated or unsaturated, aliphatic
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Paragraph 0208; 0209
(2019/01/24)
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- BENZOXAZINES WITH PHOTO-CURABLE LINKAGES, THERMOSETS THEREOF, AND PREPARATION OF THE SAME
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The subject invention provides benzoxazines with photo-curable linkages, thermosets thereof, and preparation methods of the same. The compounds of the subject invention can be used in manufacture of many kinds of cross-linking polymer material, and the obtained material is improved in terms of many properties, especially high thermal properties. Moreover, the preparation method of the subject invention can precisely synthesize the targeted products by simply steps.
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Page/Page column 12
(2021/01/12)
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- Triaryl Pyrazole Toll-Like Receptor Signaling Inhibitors: Structure–Activity Relationships Governing Pan- and Selective Signaling Inhibitors
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The immune system uses members of the toll-like receptor (TLR) family to recognize a variety of pathogen- and host-derived molecules in order to initiate immune responses. Although TLR-mediated, pro-inflammatory immune responses are essential for host defense, prolonged and exaggerated activation can result in inflammation pathology that manifests in a variety of diseases. Therefore, small-molecule inhibitors of the TLR signaling pathway might have promise as anti-inflammatory drugs. We previously identified a class of triaryl pyrazole compounds that inhibit TLR signaling by modulation of the protein–protein interactions essential to the pathway. We have now systematically examined the structural features essential for inhibition of this pathway, revealing characteristics of compounds that inhibited all TLRs tested (pan-TLR signaling inhibitors) as well as compounds that selectively inhibited certain TLRs. These findings reveal interesting classes of compounds that could be optimized for particular inflammatory diseases governed by different TLRs.
- Pollock, Julie A.,Sharma, Naina,Ippagunta, Sirish K.,Redecke, Vanessa,H?cker, Hans,Katzenellenbogen, John A.
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p. 2208 - 2216
(2018/09/25)
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- Synthesis and evaluation of hydroxychalcones as multifunctional non-purine xanthine oxidase inhibitors for the treatment of hyperuricemia
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A series of hydroxychalcone derivatives have been designed, synthesized and evaluated for human xanthine oxidase (XO) inhibitory activity. Most of the tested compounds acted moderate XO inhibition with IC50 values in the micromolar rang. Molecular docking and kinetic studies have been performed to explain the binding modes of XO with the selected compounds. In addition, in vitro antioxidant screening results indicated that some of the hydroxychalcones possessed good anti-free radical activities. Furthermore, the preferred compounds 16 and 18 were able to significantly inhibit hepatic xanthine oxidase activity and reduced serum uric acid level of hyperuricemic mice in vivo. In summary, compounds 16 and 18 with balanced activities of antioxidant, XO inhibition and serum uric acid reduction, which are promising candidates for the treatment of hyperuricemia and gout.
- Xie, Zhaodi,Luo, Xiaoting,Zou, Zhuan,Zhang, Xiao,Huang, Feifei,Li, Ruishan,Liao, Shijie,Liu, Yun
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supporting information
p. 3602 - 3606
(2017/07/07)
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- Synthesis and biological evaluation of α-methyl-chalcone for anti-cervical cancer activity
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A series of 31 chalcones were synthesized and evaluated for anti-proliferative activity against the human cervical cancer cell lines (HeLa and SiHa). Compound 19, (E)-1-(2,4-dihydroxyphenyl)-3-(4-(dimethylamino) phenyl)-2-methylprop-2-en-1-one was found to be an effective anti-proliferative agent in HeLa and SiHa cells (IC50 = 0.035 μM). Compound 19 increased the percentage of apoptosis in a dose-dependent manner, as measured by Annexin V-FITC (fluorescein isothiocyanate)/(propidium iodide) PI staining. Molecular modeling studies of compound 19 showed that the most potent structure was docked at the yeast 20 S proteasome binding site (Protein Data Bank code-3E47) and was stabilized in the cavity by various hydrophobic and hydrogen bonding interactions.
- Ren, Bing-zhao,Ablise, Mourboul,Yang, Xu-chao,Liao, Bo-er,Yang, Zheng
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p. 1871 - 1883
(2017/08/03)
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- Design, Synthesis, and Docking Study of Pyrimidine–Triazine Hybrids for GABA Estimation in Animal Epilepsy Models
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A series of new pyrimidine–triazine hybrids (4a–t) was designed and synthesized, from which potent anticonvulsant agents were identified. Most of the compounds exhibited promising anticonvulsant activity against the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) tests, along with minimal motor impairment with higher safety compared to the standard drugs, phenytoin and carbamazepine. In the series, 5-(4-(4-fluorophenyl)-6-(4-hydroxyphenyl)-2-thioxo-5,6-dihydropyrimidin-1(2H)-yl)-1,2-dihydro-1,2,4-triazin-3(6H)-one (4o) and 5-(6-(4-hydroxy-3-methoxyphenyl)-4-(4-hydroxyphenyl)-2-thioxo-5,6-dihydropyrimidin-1(2H)-yl)-1,2-dihydro-1,2,4-triazin-3(6H)-one (4s) emerged as most potent anticonvulsant agents with median doses of 22.54 and 29.40 mg/kg (MES ED50), 285.02 and 293.42 mg/kg (scPTZ ED50), and 389.11 and 412.16 mg/kg (TD50), respectively. Docking studies were also performed for all synthesized compounds to get insight into the binding pattern toward the GABAA receptor as a possible mechanism of their anticonvulsant action, and in silico ADME studies were carried out to predict the safety and stability of the molecules. The increased GABA level in the experimental animals in the neurochemical estimation assay confirmed their GABAergic modulating activity. The most potent compounds were also evaluated for their neurotoxic and hepatotoxic effects. Fortunately, they did not show any sign of neurotoxicity or hepatotoxicity, suggesting that they have a broad spectrum of anticonvulsant activity with a large safety margin. Together, this research suggested that 4o and 4s may serve as leads in the discovery and development of new anticonvulsant drugs.
- Sahu, Meeta,Siddiqui, Nadeem,Naim, Mohd. Javed,Alam, Ozair,Yar, Mohammad Shahar,Sharma, Vidushi,Wakode, Sharad
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- Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity
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A new series of monomer and dimer derivatives of dihydroartemisinin (DHA) containing substituted chalcones as a linker were synthesized and investigated for their cytotoxicity in human cancer cell lines HL-60 (leukemia), Mia PaCa-2 (pancreatic cancer), PC
- Gaur, Rashmi,Pathania, Anup Singh,Malik, Fayaz Ahmad,Bhakuni, Rajendra Singh,Verma, Ram Kishor
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p. 232 - 246
(2016/07/07)
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- Niacin esters of chalcones with tumor-selective properties
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Novel series of niacin esters of chalcones 2, 4 and 6 were designed as antineoplastic agents that have the potential to release the chemoprotectant niacin. These enones are cytotoxic to human CD4 +T-lymphocyte Molt 4/C8 and CEM and murine leukemia L1210 cells. Quantitative structure–activity relationship (QSAR) studies of the biodata in series 4 revealed that cytotoxic potency was enhanced by placing electron-repelling groups in one of the aryl rings. The compounds are lethal to HL-60, HSC-2, HSC-3 and HSC-4 neoplasms but less toxic to nonmalignant hepatocyte growth factor, hematopoietic progenitor cell and human periodontal ligament fibroblast cells. Hence, the compounds display tumor-selective toxicity. These chalcones are well tolerated in mice and no overt toxicity was noted. The results establish that in general the compounds in series 2, 4 and 6 have positive characteristics which warrant further studies.
- Panda, Atulya K.,Das, Umashankar,Roayapalley, Praveen K.,Sakagami, Hiroshi,Kawase, Masami,Balzarini, Jan,De Clercq, Erik,Dimmock, Jonathan R.
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p. 1451 - 1456
(2016/10/09)
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- 4-Fluoro-3′,4′,5′-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model
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Invasion and metastasis are responsible for 90% of cancer-related mortality. Herein, we report on our quest for novel, clinically relevant inhibitors of local invasion, based on a broad screen of natural products in a phenotypic assay. Starting from micromolar chalcone hits, a predictive QSAR model for diaryl propenones was developed, and synthetic analogues with a 100-fold increase in potency were obtained. Two nanomolar hits underwent efficacy validation and eADMET profiling; one compound was shown to increase the survival time in an artificial metastasis model in nude mice. Although the molecular mechanism(s) by which these substances mediate efficacy remain(s) unrevealed, we were able to eliminate the major targets commonly associated with antineoplastic chalcones.
- Roman, Bart I.,De Ryck, Tine,Patronov, Atanas,Slavov, Svetoslav H.,Vanhoecke, Barbara W.A.,Katritzky, Alan R.,Bracke, Marc E.,Stevens, Christian V.
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supporting information
p. 627 - 639
(2015/08/03)
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- Synthesis and biological activity of 2,4-di-p-phenolyl-6-2-furanyl-pyridine as a potent topoisomerase II poison
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Dihydroxylated 2,4-diphenyl-6-aryl pyridine derivatives were simply achieved using Claisen-Schmidt condensation reaction and modified Kr?hnke pyridine synthetic method. Total forty-five compounds were designed and synthesized which contain hydroxyl groups
- Karki, Radha,Park, Chanmi,Jun, Kyu-Yeon,Kadayat, Tara Man,Lee, Eung-Seok,Kwon, Youngjoo
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p. 360 - 378
(2015/03/18)
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- The mesomorphic properties of chalcone dimer derivatives
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A homologous series of symmetrical dimers viz bis (4-n-alkoxy benzoyloxy) -phenyl β-benzoyl-ethylenes was synthesized and studied with a view to understanding the relation between molecular structure and the mesomorphic behavior. Twelve members of the dimeric series were synthesized, and the methoxy to butyloxy homologues are not liquid crystals, but the pentyloxy to hexadecyloxy are liquid crystals. The pentyl to heptyl dimers are only nematogenic, but the higher homologues show smectogenic mesomorphism prior to nematogenic mesophase formation. The phase diagram of phase transition curves behaves in a normal manner except for the smectic to nematic transition curve which behaves in an unexpected manner. The smectic and nematic thermal stabilities are 103°C and 131.7°C, respectively. The smectogenic and nematogenic phase lengths vary between 17.4°C to 28.3°C and 2.1°C to 29.9°C, respectively. The liquid crystal properties of presently investigated novel chalcone dimers are compared with known monomeric chalcones.
- Kotadiya,Bhoya
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p. 116 - 124
(2015/03/18)
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- Synthesis and biological activity of 2,4-di- p -phenolyl-6- 2 -furanyl-pyridine as a potent topoisomerase II poison
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Dihydroxylated 2,4-diphenyl-6-aryl pyridine derivatives were simply achieved using Claisen-Schmidt condensation reaction and modified Kr?hnke pyridine synthetic method. Total forty-five compounds were designed and synthesized which contain hydroxyl groups
- Karki, Radha,Park, Chanmi,Jun, Kyu-Yeon,Kadayat, Tara Man,Lee, Eung-Seok,Kwon, Youngjoo
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p. 360 - 378
(2015/02/19)
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- Functionalized curcumin analogs as potent modulators of the Wnt/β-catenin signaling pathway
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Osteosarcoma is a primary bone malignancy with aggressive metastatic potential and poor prognosis rates. In our earlier work we have investigated the therapeutic potential of curcumin as an anti-invasive agent in osteosarcoma by its ability to regulate the Wnt/β-catenin signaling pathway. However, the clinical use of curcumin is limited owing to its low potency and poor pharmacokinetic profile. In this study, an attempt was made to achieve more potent Wnt inhibitory activity in osteosarcoma cells by carrying out synthetic chemical modifications of curcumin. We synthesized a total of five series consisting of 43 curcumin analogs and screened in HEK293T cells for inhibition of β-catenin transcriptional activity. Six promising analogs, which were 6.5- to 60-fold more potent than curcumin in inhibiting Wnt activity, were further assessed for their anti-invasive activity and Wnt inhibitory mechanisms. Western blot analysis showed disruption of β-catenin protein nuclear translocation following treatment with analogs 2f, 3c and 4f. Using transwell assays, we also found that these compounds were more potent than 1a (curcumin) in impeding the invasion of osteosarcoma cells, possibly through suppressing MMP-9 activity. Structure-activity-relationship studies revealed that Wnt inhibitory effects could be enhanced by shortening and restraining the flexibility of the 7-carbon linker moiety connecting the terminal aromatic rings of curcumin and substituting both rings with appropriate substituents. Our results demonstrate that the synthesized curcumin analogs are more potent Wnt inhibitors in osteosarcoma cell lines as compared to parental curcumin and are good lead compounds for further development. Future in vivo tests with these compounds will define their therapeutic potentials as promising drug candidates for clinical treatment of osteosarcoma.
- Leow, Pay-Chin,Bahety, Priti,Boon, Choon Pei,Lee, Chong Yew,Tan, Kheng Lin,Yang, Tianming,Ee, Pui-Lai Rachel
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- Nano titania-supported sulfonic acid: An efficient and reusable catalyst for a range of organic reactions under solvent free conditions
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Nano titania-supported sulfonic acid (n-TSA) has been easily prepared from the reaction of nano titania (titanium oxide) with chlorosulfonic acid as sulfonating agent and characterized by the FT-IR spectroscopy, scanning electron microscopy (SEM), X-ray diffraction (XRD) and thermal gravimetric analysis (TGA). The catalytic activity of n-TSA was investigated in the synthesis of important organic derivatives such as pyrimidones, benzothiazoles and chalcones. All of the reactions are very fast and the yields are good to excellent. The catalyst was easily separated and reused for several runs without appreciable loss of its catalytic activity.
- Rahmani, Salman,Amoozadeh, Ali,Kolvari, Eskandar
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p. 184 - 188
(2014/11/08)
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- Discovery of dihydroxylated 2,4-diphenyl-6-thiophen-2-yl-pyridine as a non-intercalative DNA-binding topoisomerase II-specific catalytic inhibitor
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We describe our rationale for designing specific catalytic inhibitors of topoisomerase II (topo II) over topoisomerase I (topo I). Based on 3D-QSAR studies of previously published dihydroxylated 2,4-diphenyl-6-aryl pyridine derivatives, 9 novel dihydroxyl
- Jun, Kyu-Yeon,Kwon, Hanbyeol,Park, So-Eun,Lee, Eunyoung,Karki, Radha,Thapa, Pritam,Lee, Jun-Ho,Lee, Eung-Seok,Kwon, Youngjoo
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p. 428 - 438
(2014/05/20)
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- Total synthesis and assignment of the absolute stereochemistry of xanthoangelol J: Development of a highly efficient method for Claisen-Schmidt condensation Dedicated to Late (Dr.) Jadab C. Sarma on his 55th birthday on first May 2013
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The first total synthesis of cancer chemopreventive terpenyl hydroxychalcone xanthoangelol J isolated from Angelica keiskei was accomplished with asymmetric epoxidation, aromatic C-alkylation and Claisen-Schmidt condensation via enol mode as key steps. The crucial Claisen-Schmidt condensation has been accomplished by a novel green method using KHSO 4-SiO2 as a recyclable catalyst under microwave activation. The absolute configuration of the molecule was also determined.
- Kakati, Dwipen,Barua, Nabin C.
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p. 637 - 642
(2014/02/14)
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- Design and synthesis of 3,5-diaryl-4,5-dihydro-1H-pyrazoles as new tyrosinase inhibitors
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In this study, twenty 3,5-diaryl-4,5-dihydro-1H-pyrazole derivatives with hydroxyl(s) (1a-1p, 2a-2d) were synthesized and their inhibitory activity on mushroom tyrosinase was examined. The results showed that among these compounds, 1-(5-(3,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl) ethanone 1d was found to be the most potent tyrosinase inhibitor with IC 50 value of 0.301 μM. Kinetic study revealed that these compounds were competitive inhibitors of tyrosinase and their structure-activity relationships were investigated in this article.
- Zhou, Zhixuan,Zhuo, Jiaru,Yan, Sujun,Ma, Lin
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p. 2156 - 2162
(2013/05/08)
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- Inhibitory effect of curcumin analogs on tissue factor procoagulant activity and their preliminary structure-activity relationships
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With the aim to explore the multifunctional behaviors of curcumin analogs and to discover new small molecular tissue factor inhibitors, twelve mono carbonyl curcumin analogs of three classes were synthesized and their effect on tissue factor procoagulant activity was evaluated in the human monoblastic leukemia THP-1 cells stimulated by LPS. The most potent compounds 2a exhibited the dramatically enhanced activity with the IC50 values of 0.053 nM. Their preliminary structure-activity relationship was also discussed.
- Ge, Hai-Xia,Chen, Ling,Zhang, Jian,Kou, Jun-Ping,Yu, Bo-Yang
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p. 3242 - 3246
(2013/07/27)
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- Dihydroxylated 2,4,6-triphenyl pyridines: Synthesis, topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study
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Twelve dihydroxylated 2,4,6-triphenyl pyridines were designed and synthesized which contain hydroxyl groups at ortho, meta or para position of 2- and 6-phenyl, or 2- and 4-phenyl rings attached to the central pyridine. They were evaluated for topoisomeras
- Karki, Radha,Thapa, Pritam,Yoo, Han Young,Kadayat, Tara Man,Park, Pil-Hoon,Na, Youngwha,Lee, Eunyoung,Jeon, Kyung-Hwa,Cho, Won-Jea,Choi, Heesung,Kwon, Youngjoo,Lee, Eung-Seok
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experimental part
p. 219 - 228
(2012/05/05)
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- Synthesis of norlignans and in vitro inhibitory activity of antigen-induced degranulation
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The synthesis and biological evaluation of a series of novel norlignans are described. Norlignans were evaluated for their inhibitory activity on the release of β-hexosaminidase, a marker of degranulation, from RBL-2H3 cells induced by the IgE-antigen com
- Park, Eonjeong,Yang, Yoon Jung,Kim, Aejin,Kwak, Jong Hwan,Jung, Young Hoon,Kang, Se Chan,Kim, In Su
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supporting information; body text
p. 3653 - 3655
(2012/07/16)
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- Synthesis and topoisomerase II inhibitory and cytotoxic activity of oxiranylmethoxy- and thiiranylmethoxy-chalcone derivatives
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In order to find potential anticancer drug candidate targeting topoisomerases enzyme, we have designed and synthesized oxiranylmethoxy- and thiiranylmethoxy-retrochalcone derivatives and evaluated their pharmacological activity including topoisomerases inhibitory and cytotoxic activity. Of the compounds prepared compound 25 showed comparable or better cytotoxic activity against cancer cell lines tested. Compound 25 inhibited MCF7 (IC50: 0.49 ± 0.21 μM) and HCT15 (IC50: 0.23 ± 0.02 μM) carcinoma cell growth more efficiently than references. In the topoisomerases inhibition test, all the compounds were inactive to topoisomerase I but moderate inhibitors to topoisomerase II enzyme. Especially, compound 25 inhibited topoisomerase II activity with comparable extent to etoposide at 100 μM concentrations. Correlation between cytotoxicity and topoisomerase II inhibitory activity implies that compound 25 can be a possible lead compound for anticancer drug impeding the topoisomerase II function.
- Na, Younghwa,Nam, Jung-Min
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scheme or table
p. 211 - 214
(2011/02/25)
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- Comparative study of conventional and microwave assisted synthesis of chalcones
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An efficient, facile and eco-friendly microwave assisted approach for the synthesis of substituted chalcones by condensation of substituted acetophenones with substituted benzaldehyds in presence of an inorganic base is desired over time consuming convent
- Sharma, Bhavana
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experimental part
p. 2468 - 2470
(2012/01/14)
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- Synthesis and evaluation of some new substituted benzothiazepine and benzoxazepine derivatives as anticonvulsant agents
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A new series of 4-(4′-Hydroxyphenyl)-2-(3-substitutedphenyl)-3-(4-substitutedphenylamino methylene)-2,3-dihydro-1,5-benzothiazepines (3a-3j) and 4-(4′-Hydroxyphenyl)-2-(3-substituted phenyl)-3-(4-substitutedphenylaminomethylene)-2,3-dihydro-1,5-benzoxazep
- Garg, Neha,Chandra, Trilok,Archana,Jain, Amit B.,Kumar, Ashok
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experimental part
p. 1529 - 1535
(2010/06/14)
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- Evaluation of anti-pigmentary effect of synthetic sulfonylamino chalcone
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The 4′-(p-toluenesulfonylamino)-4-hydroxychalcone (TSAHC), which bears inhibitory chemotypes for both α-glucosidase and tyrosinase, was evaluated for tyrosinase activity and depigmenting ability relative to compounds designed to only target tyrosianse act
- Seo, Woo Duck,Ryu, Young Bae,Curtis-Long, Marcus J.,Lee, Chan Woo,Ryu, Hyung Won,Jang, Ki Chang,Park, Ki Hun
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experimental part
p. 2010 - 2017
(2010/07/04)
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- Synthesis and evaluation of antiinflammatory activity of substituted chalcone derivatives
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In an effort to develop potent antiinflammatory agents, a series of substituted chalcone derivatives was synthesized and evaluated for antiinflammatory activity through monitoring of their ability to inhibit xylene-induced ear edema in mice. Some of the tested compounds exhibited significant activity, and compounds 3f [(E)-1-(2,4-dihydroxyphenyl)-3-(4- dimethylamino)phenyl)prop-2-en-1-one] and 3h [(E)-3-(4-chlorophenyl)-1-(2,4- dihydroxyphenyl)prop-2-en-1-one] showed the highest antiinflammatory activity (62 and 68% inhibition, respectively, 2 h before administration), comparable with or even slightly more potent than the reference drug ibuprofen (53%). Furthermore, the structure-activity relationship of these substituted chalcone derivatives was demonstrated.
- Zhang, Xue-Wu,Zhao, Dong-Hai,Quan, Ying-Chun,Sun, Liang-Peng,Yin, Xiu-Mei,Guan, Li-Ping
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experimental part
p. 403 - 412
(2011/02/27)
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- Chemoselective regulation of TREK2 channel: Activation by sulfonate chalcones and inhibition by sulfonamide chalcones
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Although it has not been extensively studied, a significant volume of literature suggests that TREK2 will probably turn out to be an important channel in charge of tuning neuronal transmitter and hormone levels. Thus, pharmacological tools which can manip
- Kim, Eun-Jin,Ryu, Hyung Won,Curtis-Long, Marcus J.,Han, Jaehee,Kim, Jun Young,Cho, Jung Keun,Kang, Dawon,Park, Ki Hun
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supporting information; experimental part
p. 4237 - 4239
(2010/08/22)
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- NaOAc-mediated selective deprotection of aromatic acetates and Its application in the synthesis of natural products
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We have developed an efficient method to deacetylate the aromatic acetates using NaOAc in excellent yields and demonstrated the application of the procedure in the synthesis of natural products.
- Narender,Reddy, K. Papi,Madhur
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experimental part
p. 1949 - 1956
(2009/10/17)
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- Pyrazoline-based mycobactin analogues as MAO-inhibitors
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3,5-Diaryl carbothioamide pyrazolines designed as mycobactin analogs (mycobacterial siderophore) were reported to be potent antitubercular agents under iron limiting condition in our earlier study. Clinical complications of newly introduced antibiotic Linezolid, due its MAO inhibitory activity, prompted us to evaluate our compounds for their MAO-inhibitory activity against rat liver MAO-A and MAO-B as pyrazolines were reported to be antidepressants and MAO inhibitors. The present study carried out with this pilot library of 32 compounds will provide us with necessary information for designing antitubercular molecules with reduced MAO-inhibitory activity and also help us in identifying a selective MAO-B inhibitor which has potential clinical utility in neurodegenerative disorders. Thirty-two compounds analyzed has shown spectrum of activity from selective to nonselective against two isoforms of rat liver MAO-A and MAO-B and also as competitive, reversible to non-competitive, irreversible. It is also interesting to note that anti-tubercular compound 11, 14 and 16 were also found to be selective inhibitors of rat liver MAO-B. Docking studies with human MAO shows that compound 11 interacts with the catalytic site of both the isoforms, suggesting compound 11 as nonselective inhibitor of human MAO isoforms.
- Jayaprakash, Venkatesan,Sinha, Barij N.,Ucar, Gulberk,Ercan, Ayse
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scheme or table
p. 6362 - 6368
(2009/09/30)
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- Small molecules with structural similarities to siderophores as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis
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Drugs inhibiting the iron scarcity-induced, siderophore-mediated iron-scavenging systems of Mycobacterium tuberculosis (Mtb) and Yersinia pestis (Yp) may provide new therapeutic lines of defense. Compounds with structural similarities to siderophores were synthesized and evaluated as antimicrobials against Mtb and Yp under iron-limiting conditions, which mimic the iron scarcity these pathogens encounter and must adapt to in the host, and under standard iron-rich conditions for comparison. New antimicrobials were identified, some of which warrant exploration as initial leads against potentially novel targets and small-molecule tools to assist in the elucidation of targets specific to iron-scarcity adapted Mtb and Yp.
- Stirrett, Karen L.,Ferreras, Julian A.,Jayaprakash, Venkatesan,Sinha, Barij N.,Ren, Tao,Quadri, Luis E.N.
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p. 2662 - 2668
(2008/12/21)
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- NOVEL CHALCONE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALT, METHOD FOR PREPARATION AND USES THEREOF
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Disclosed relates to a novel chalcone derivative, pharmaceutically acceptable salt thereof, a method for preparing the same and uses thereof, the chalcone derivative being readily obtained through the steps of : reacting aminoacetophenone with sulfonylchl
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Page/Page column 28-29
(2008/06/13)
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- Microwave-Accelerated SPOT-synthesis on cellulose supports
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Equation presented. We demonstrate that microwave irradiation can dramatically accelerate reaction rates for spatially addressable library synthesis on planar membrane supports. The development of a robust support/linker system, microwave-assisted synthesis of small molecule test libraries, and methods for solid-phase scale-up on cellulose are described.
- Bowman, Matthew D.,Jeske, Ryan C.,Blackwell, Helen E.
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p. 2019 - 2022
(2007/10/03)
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- Demand-based thiolate anion generation under virtually neutral conditions: Influence of steric and electronic factors on chemo- and regioselective cleavage of aryl alkyl ethers
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Thiolate anions have been generated in a "demand-based" fashion under virtually neutral conditions for chemoselective deprotection of aryl alkyl ethers. Solvents play the critical role in making the reaction effective and should have high values of ε (>30), molecular polarizabilities (>10), and DN (>27) and low values of AN (>14). However, it is the combined effect of all of these physical properties that make a particular solvent effective. The reaction rates of cleavage of various aryl alkyl ethers are dependent on the steric crowding around the O-alkyl carbon and follow the order propargyl ≈ allyl ≈ benzyl > methyl > ethyl. Electron-withdrawing substituents increase the rate of ether cleavage reaction. The influence of the steric and electronic factors have been successfully exploited for selective deprotection of aryl alkyl ethers during inter- and intramolecular competitions.
- Chakraborti, Asit K.,Sharma, Lalima,Nayak, Mrinal K.
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p. 6406 - 6414
(2007/10/03)
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- Synthesis and description of chalcone-like compounds, inhibitors of aldose reductase
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A series of hydroxy- and hydroxy-methoxychalcones was synthesized and the inhibitory activity and selectivity of the compounds towards bovine lens aldose reductase (AR) were tested. All the compounds display affinity for AR. The most active proved to be 1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)propen-1-one (isoliquiritigenin, IC50= 7.60 μM). The selectivity of this compound was also tested, its inhibitory activity being assayed against glutathione reductase and sorbitol dehydrogenase.
- Severi,Costantino,Benvenuti,Vampa,Mucci
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p. 128 - 136
(2007/10/03)
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- Antitumorigenic activities of chalcones. I. Inhibitory effects of chalcone derivatives on 32Pi-incorporation into phospholipids of HeLa cells promoted by 12-O-tetradecanoyl-phorbol 13-acetate (TPA)
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More than forty chalcone derivatives were synthesized to examine their structure-activity relationship against tumorigenesis. As a primary screening test, the inhibitory activities of the chalcones for the 32pi-incorporation into phospholipids of HeLa cells enhanced by 12-O-tetradecanoyl-phorbol 13- acetate (TPA) were examined. 3-Hydroxy-chalcone derivatives possessing methyl group in 3'-, 4'-, or 2'-position and isoliquiritigenin homologs showed potent inhibitory activities in the phosphorylation test, which suggests their antitumorigenic effects.
- Iwata,Nishino,Nagata,Satomi,Nishino,Shibata
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p. 1710 - 1713
(2007/10/03)
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- Microwave-assisted Deacetylation on Alumina: a Simple Deprotection Method
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A simple high-yielding method for the deprotection of acetylated phenols and alcohols is described which occurs under mild conditions on an alumina surface using microwave irradiation.
- Varma, Rajender S.,Varma, Manju,Chatterjee, Arnab K.
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p. 999 - 1000
(2007/10/02)
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- SYNTHESIS OF LIQUID CRYSTALLINE 3,5-DIARYL 1,2-DITHIOLIUM SALTS
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The title compounds are obtained by heterocyclisation of dialkoxy substituted diaryl β-diketones or chalcones using P4S10.
- Veber, M.,Jallabert, C.,Strzeleska, H.
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p. 693 - 702
(2007/10/02)
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- Process for treating inflammation
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A process for treating inflammation locally or topically by administering a compound of the formula: STR1 wherein M and M' are hydrogen, hydroxy, halogen, lower alkyl of from 1 to 3 carbon atoms, lower alkoxy of from 1 to 3 carbon atoms; NH2, R
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