- A NIR light-triggered drug delivery system using core-shell gold nanostars-mesoporous silica nanoparticles based on multiphoton absorption photo-dissociation of 2-nitrobenzyl PEG
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Gold nanostars coated with a mesoporous silica shell and functionalized with poly(ethylene glycol) containing photolabile 2-nitrobenzyl moieties are able to release doxorubicin after NIR light irradiation at low power irradiance via a multiphoton absorpti
- Hernández-Montoto, Andy,Gorbe, Mónica,Llopis-Lorente, Antoni,Terrés, José Manuel,Montes, Roberto,Cao-Milán, Roberto,Díaz De Gre?u, Borja,Alfonso, María,Orzaez, Mar,Marcos, María Dolores,Martínez-Má?ez, Ramón,Sancenón, Félix
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Read Online
- Curcumin-based fluorescent chemosensor for selective and efficient detection of picric acid
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We developed a curcumin-based chemosensor (DCD) for selective and efficient detection of Picric acid (PA). The developed chemosensor DCD exhibit a broad emission band at 516 nm and shows green colour fluorescence in DMSO/H2O solution (8:2, v/v)
- Madhu,Sivakumar
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Read Online
- 3-hydroxycurcumin-4-OCH2CO2H strontium, and synthesis, activity and application thereof
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The invention discloses 3-hydroxycurcumin-4-OCH2CO2H strontium, discloses a preparation method of the 3-hydroxycurcumin-4-OCH2CO2H strontium, and discloses anti-osteoporosis activity of the 3-hydroxycurcumin-4-OCH2CO2H strontium so that the invention disc
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Paragraph 0012; 0014-0015
(2020/12/14)
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- Targeting receptor tyrosine kinase VEGFR-2 in hepatocellular cancer: Rational design, synthesis and biological evaluation of 1,2-disubstituted benzimidazoles
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In this study, a novel series of 1,2-disubstituted benzo[d]imidazoles was rationally designed as VEGFR-2 inhibitors targeting hepatocellular carcinoma. Our design strategy is twofold; it aimed first at studying the effect of replacing the 5-methylfuryl moiety of the well-known antiangiogenic 2-furylbenzimidazoles with an isopropyl moiety on the VEGFR-2 inhibitory activity and the cytotoxic activity. Our second objective was to further optimize the structures of the benzimidazole derivatives through elongation of the side chains at their one-position for the design of more potent type II-like VEGFR-2 inhibitors. The designed 1,2-disubstituted benzimidazoles demonstrated potent cytotoxic activity against the HepG2 cell line, reaching IC50 = 1.98 μM in comparison to sorafenib (IC50 = 10.99 μM). In addition, the synthesized compounds revealed promising VEGFR-2 inhibitory activity in the HepG2 cell line, e.g., compounds 17a and 6 showed 82% and 80% inhibition, respectively, in comparison to sorafenib (% inhibition = 92%). Studying the effect of 17a on the HepG2 cell cycle demonstrated that 17a arrested the cell cycle at the G2/M phase and induced a dose-dependent apoptotic effect. Molecular docking studies of the synthesized 1,2-disubstituted benzimidazoles in the VEGFR-2 active site displayed their ability to accomplish the essential hydrogen bonding and hydrophobic interactions for optimum inhibitory activity.
- Abdel-Mohsen, Heba T.,Abdullaziz, Mona A.,Ali, Mamdouh M.,El Diwani, Hoda I.,El Kerdawy, Ahmed M.,Flanagan, Keith J.,Mahmoud, Abeer E. E.,Ragab, Fatma A. F.,Senge, Mathias O.
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- Janus Gold Nanostars–Mesoporous Silica Nanoparticles for NIR-Light-Triggered Drug Delivery
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Janus gold nanostar–mesoporous silica nanoparticle (AuNSt–MSNP) nanodevices able to release an entrapped payload upon irradiation with near infrared (NIR) light were prepared and characterized. The AuNSt surface was functionalized with a thiolated photolabile molecule (5), whereas the mesoporous silica face was loaded with a model drug (doxorubicin) and capped with proton-responsive benzimidazole-β-cyclodextrin supramolecular gatekeepers (N 1). Upon irradiation with NIR-light, the photolabile compound 5 photodissociated, resulting in the formation of succinic acid, which induced the opening of the gatekeeper and cargo delivery. In the overall mechanism, the gold surface acts as a photochemical transducer capable of transforming the NIR-light input into a chemical messenger (succinic acid) that opens the supramolecular nanovalve. The prepared hybrid nanoparticles were non-cytotoxic to HeLa cells, until they were irradiated with a NIR laser, which led to intracellular doxorubicin release and hyperthermia. This induced a remarkable reduction in HeLa cells viability.
- Hernández Montoto, Andy,Llopis-Lorente, Antoni,Gorbe, Mónica,M. Terrés, José,Cao-Milán, Roberto,Díaz de Gre?u, Borja,Alfonso, María,Iba?ez, Javier,Marcos, María D.,Orzáez, Mar,Villalonga, Reynaldo,Martínez-Má?ez, Ramón,Sancenón, Félix
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p. 8471 - 8478
(2019/07/16)
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- Iridium-catalysed primary alcohol oxidation and hydrogen shuttling for the depolymerisation of lignin
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Lignin is a potentially abundant renewable resource for the production of aromatic chemicals, however its selective depolymerisation is challenging. Here, we report a new catalytic system for the depolymerisation of lignin to novel, non-phenolic monoaromatic products based on the selective β-O-4 primary alcohol dehydrogenation with a Cp?Ir-bipyridonate catalyst complex under basic conditions. We show that this system is capable of promoting the depolymerisation of model compounds and isolated lignins via a sequence of selective primary alcohol dehydrogenation, retro-aldol (Cα-Cβ) bond cleavage and in situ stabilisation of the aldehyde products by transfer (de)hydrogenation to alcohols and carboxylic acids. This method was found to give good to excellent yields of cleavage products with both etherified and free-phenolic lignin model compounds and could be applied to real lignin to generate a range of novel non-phenolic monomers including diols and di-acids. We additionally show, by using the same catalyst in a convergent, one-pot procedure, that these products can be selectively channelled towards a single di-acid product, giving much simpler product mixtures as a result.
- Lancefield, Christopher S.,Teunissen, Lucas W.,Weckhuysen, Bert M.,Bruijnincx, Pieter C. A.
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p. 3214 - 3221
(2018/07/31)
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- Lys modification of curcumin derivatives, their synthesis and use
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The present invention discloses pseudo-peptides as the following formula, and further discloses a preparation method and applications of the pseudo-peptides. The pseudo-peptides in the invention have an excellent thrombolytic activity, an antithrombotic a
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Paragraph 0037; 0040; 0041
(2018/11/03)
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- Pharmacological protection of mitochondrial function mitigates acute limb ischemia/reperfusion injury
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We describe several novel curcumin analogues that possess both anti-inflammatory antioxidant properties and thrombolytic activities. The therapeutic efficacy of these curcumin analogues was verified in a mouse ear edema model, a rat arterial thrombosis as
- Bi, Wei,Bi, Yue,Gao, Xiang,Yan, Xin,Zhang, Yanrong,Harris, Jackie,Legalley, Thomas D.,Gibson, K. Michael,Bi, Lanrong
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supporting information
p. 4042 - 4051
(2016/08/01)
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- The synthesis and analysis of advanced lignin model polymers
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If the lignin-first biorefinery concept becomes a reality, high quality lignins close in structure to native lignins will become available in large quantities. One potential way to utilise this renewable material is through depolymerisation to aromatic chemicals. This will require the development of new chemical methods. Here, we report the synthesis and characterisation of advanced lignin model polymers to be used as tools to develop these methods. The controlled incorporation of the major linkages in lignin is demonstrated to give complex hardwood and softwood lignin model polymers. These polymers have been characterised by 2D HSQC NMR and GPC analysis and have been compared to isolated lignins.
- Lancefield,Westwood
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supporting information
p. 4980 - 4990
(2015/11/16)
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- Isolation of functionalized phenolic monomers through selective oxidation and CO bond cleavage of the β-O-4 linkages in Lignin
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Functionalized phenolic monomers have been generated and isolated from an organosolv lignin through a two-step depolymerization process. Chemoselective catalytic oxidation of β-O-4 linkages promoted by the DDQ/tBuONO/ O2 system was achieved in model compounds, including polymeric models and in real lignin. The oxidized β-O-4 linkages were then cleaved on reaction with zinc. Compared to many existing methods, this protocol, which can be achieved in one pot, is highly selective, giving rise to a simple mixture of products that can be readily purified to give pure compounds. The functionality present in these products makes them potentially valuable building blocks.
- Lancefield, Christopher S.,Ojo, O. Stephen,Tran, Fanny,Westwood, Nicholas J.
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supporting information
p. 258 - 262
(2015/02/19)
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- Synthesis of a photocaged tamoxifen for light-dependent activation of Cre-ER recombinase-driven gene modification
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We report the design of a water-soluble, quaternized tamoxifen photoprobe and demonstrate its application in light-controlled induction of green fluorescent protein expression via a Cre-ER recombinase system. The Royal Society of Chemistry.
- Inlay, Matthew A.,Choe, Veronica,Bharathi, Sophia,Fernhoff, Nathaniel B.,Baker, James R.,Weissman, Irving L.,Choi, Seok Ki
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p. 4971 - 4973
(2013/07/04)
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- Potash alum [KAL(SO4)2.12H2O] catalysed esterification of formylphenoxyaliphatic acids
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A convenient and clean procedure for esterification is reported. Direct condensation of formylphenoxyaliphatic acids with low to high boiling alcohols catalysed by potash alum gave moderate to good yields. This catalyst could be recovered and reused without substantial loss in its catalytic activity and the methodology could be used for a range of closely related substrates.
- Shunmugadhas, Ganesan,Kumar, Suresh,Kumaresan, Sudalaiandi
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p. 857 - 863,7
(2020/09/09)
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- HYPOPHOSPHOROUS ACID DERIVATIVES HAVING ANTIHYPERALGIC ACTIVITY AND BIOLOGICAL APPLICATIONS THEREOF
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The invention relates to hypophosphorous acid derivatives of formula (I) wherein - X is H or OH, - R represents one or several radicals R1-R5, identical or different, two of R1-R5 optionally occupying the same position on the phenyl group, one to four of R1-R5 being H and the others being selected in the group comprising - 0-(CH2)n-COOH; - S-(CH2)n-COOH; -NH-(CH2)n-COOH; - 0-(CH,R') -COOH; -O- (CH2)n-OH; OR', -R' being a C1 -C3 alkyl radical;-OH; --COOH; halogen, particularly -F, - CI, -Br, -I, -CF3; -OCF3; -N02; -CH=CH-COOH; - -(CH2)n-COOH; O - (CH2)n- P03H2; O - (CF2)n- P03H2; O - (CH2)n- S03H; O - (CH2)n- CONHOH; O - (CH2)n-tetrazol; O - (CH2)n-hydroxyisoxazol - n = 1 to 5, preferably 1-3; said hypophosrous acid derivatives being diastereoisomers or enantiomers.
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(2012/12/13)
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- A concise asymmetric synthesis of (-)-virolin, (-)-surinamensin,(-)- raphidecursinol B and (-)-polysphorin
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Highly concise and general asymmetric syntheses of biologically important natural (-)-8,4-oxyneolignans [(-)-virolin, (-)-surinamensin, (-)-raphidecursinol B, and (-)-polysphorin] are reported. The key step in the synthesis is the Evan's syn-aldol reaction to achieve the adducts with the desired stereochemistry. The four biologically important plant metabolites were synthesized using two common intermediates. Georg Thieme Verlag Stuttgart · New York.
- Nagaraju, Manda,Chandra, Rajesh,Gawali, Bhimrao B.
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supporting information; experimental part
p. 1485 - 1488
(2012/07/28)
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- A green chemistry method for the regeneration of carbonyl compounds from oximes by using cupric chloride dihydrate as a recoverable promoter for hydrolysis
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A mild, efficient, general, and green method for the regeneration of carbonyl compounds from their corresponding oximes is described. Cupric salts promoted hydrolysis of oximes was studied, and the best reaction conditions for the hydrolysis have been found. Carbonyl compounds were obtained in 85-98% yields after the treatment of oximes with 2 molar equivalent of CuCl 22H2O at reflux (around 75 C) in a mixed solvent of acetonitrile and water (4:1). In addition, cupric salt was readily recovered in an almost quantitative yield via the complete precipitation of Cu(OH) 22H2O. Georg Thieme Verlag Stuttgart · New York.
- Quan, Na,Shi, Xiao-Xin,Nie, Liang-Deng,Dong, Jing,Zhu, Rui-Heng
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experimental part
p. 1028 - 1032
(2011/06/17)
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- Light-controlled release of caged doxorubicin from folate receptor-targeting PAMAM dendrimer nanoconjugate
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We report the synthesis and in vitro evaluation of folate receptor-targeted nanoconjugate that releases its therapeutic payload via a photochemical mechanism.
- Ki Choi, Seok,Thomas, Thommey,Li, Ming-Hsin,Kotlyar, Alina,Desai, Ankur,Baker Jr., James R.
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supporting information; experimental part
p. 2632 - 2634
(2010/07/08)
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- DIMERIC CYANOACRYLATE COMPOUNDS AS RED-SHIFTED UV ABSORBERS
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Dimeric cyanoacrylate compounds of Formula (I) and Formula (II) having low volatility are provided for absorption of radiation in the UV-A region of the electromagnetic spectrum, which encompasses wavelengths between 320 nm and 400 nm. These compounds can
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(2010/06/15)
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- BENZENE DERIVATIVES,PROCESS FOR PREPARING THE SAME AND USE THEREOF
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Novel benzene derivatives represented by the formula (I) : wherein R1, R4 and R6 each independently represents a hydrogen atom, a halogen atom or a hydrocarbon group, R2 represents a hydrocarbon group or a heterocyclic group, R3 represents a hydrocarbon group, NR7'R7 or OR8 (wherein R7' represents a hydrogen atom or a hydrocarbon group, R7 represents a non-aromatic group, or R7' and R7 may form a ring with the adjacent nitrogen atom, and R8 represents a hydrocarbon group or a heterocyclic group), R5 represents a hydrocarbon group or a heterocyclic group (except for a quinolyl group), R5' represents a hydrogen atom, or a hydrocarbon group, or R5 and R5' may form a ring with the adjacent nitrogen atom, and R5" represents a hydrogen atom or a hydrocarbon group, which have vanilloid receptor agonist activity and are useful as a drug such as an analgesic and an agent for preventing and/or treating urinary frequency and/or urinary incontinence.
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(2010/02/07)
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- Lignin Peroxidase-Catalyzed Oxidation of Nonphenolic Trimeric Lignin Model Compounds: Fragmentation Reactions in the Intermediate Radical Cations
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The H2O2-promoted oxidations of the two nonphenolic β-O-aryl lignin model trimers 1 and 2, catalyzed by lignin peroxidase (LiP) at pH = 3.5, have been studied. The results have been compared with those obtained in the oxidation of 1 and 2 with the genuine one-electron oxidant potassium 12-tungstocobalt(III)ate. These models present a different substitution pattern of the three aromatic rings, and by one-electron oxidation, they form radical cations with the positive charge, which is localized in the dialkoxylated ring as also evidenced by a pulse radiolysis study. Both the oxidations with the enzymatic and with the chemical systems lead to the formation of products deriving from the cleavage of C-C and C-H bonds in a β position with respect to the radical cation with the charge residing in the dialkoxylated ring (3,4-dimethoxybenzaldehyde (5) and a trimeric ketone 6 in the oxidation of 1 and a dimeric aldehyde 8 and a trimeric ketone 9 in the oxidation of 2). These products are accompanied by a dimeric aldehyde 7 in the oxidation of 1 and 4-methoxybenzaldehyde (10) in the oxidation of 2. The unexpected formation of these two products has been explained by suggesting that 1.+ and 2.+ can also undergo an intramolecular electron transfer leading to the radical cations 1a.- and 2a .+ with the charge residing in a monoalkoxylated ring. The fast cleavage of a C-C bond β to this ring, leading to 7 from 1.+ and to 10 from 2.+, is the driving force of the endoergonic electron transfer. A kinetic steady-state investigation of the LiP-catalyzed oxidation of the trimer 2, the dimeric model 1-(3,4-dimethoxyphenyl)-2-phenoxy-1-ethanol (4), and 3,4-dimethoxybenzyl alcohol (3) has indicated that the turnover number (kcat) and the affinity for the enzyme decrease significantly by increasing the size of the model compound. In contrast, the three substrates exhibited a very similar reactivity toward a chemical oxidant [Co IIIW]. This suggests a size-dependent interaction of the enzyme with the substrate which may influence the efficiency of the electron transfer.
- Baciocchi, Enrico,Fabbri, Claudia,Lanzalunga, Osvaldo
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p. 9061 - 9069
(2007/10/03)
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- 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations
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The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:
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- 2-PHENYL-1-[4-(2-AMINOETHOXY)-BENZYL]-INDOLES AS ESTROGENIC AGENTS
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The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below: STR1
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- Chalcone derivatives
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The present invention provides chalcone derivatives of the general formulae: STR1 wherein R1 is a hydroxyl, carboxylic or sulphonic acid group or a carboxyalkoxy or sulphoalkoxy radical, R2 is an unsaturated, straight-chained or bran
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- Chalcone derivatives
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The present invention provides new chalcone derivatives of the general formula: STR1 wherein R1 is a hydroxyl, carboxylic acid or sulphonic acid group or a carboxyalkoxy or sulphoalkoxy radical, R2 and R3, which may be the same or different, are hydrogen or halogen atoms, hydroxyl groups or alkoxy radicals and R4 is an alkyl, hydroxyalkyl, alkoxy, carboxyalkoxy, sulphoalkoxy or carboxyalkylcarbonyloxyalkyl radical or a carboxylic acid or sulphonic acid group, with the proviso that compounds of general formula (Ia) always contain at least one carboxylic acid or sulphonic acid group; and the non-toxic inorganic and organic salts of those compounds containing at least one carboxylic acid or sulphonic acid group, the compounds of the invention are useful for treating inflammatory and allergic conditions and for treating ulcerous conditions of the gastro-intestinal tract in humans.
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