Showing papers in "Bioorganic & Medicinal Chemistry in 2000"

TL;DR: Tyrosinase inhibitory activity of flavonols, galangin, kaempferol and quercetin, was found to come from their ability to chelate copper in the enzyme, in contrast to the corresponding flavones, chrysin.

TL;DR: In this paper, a number of new benzimidazole derivatives were synthesized and their pharmacological activities were examined, including a good suppressive action on histamine release from rat peritoneal mast cells produced by antigen-antibody reaction, an antagonistic action on guinea pig ileum contraction caused by histamine, an inhibitory action on 5-lipoxygenase in rat basophilic leukemia-1 (RBL-1) cells, and a preventive action on NADPH dependent lipid peroxidation induced by Fe3+-ADP

TL;DR: This review tries to summarize the latest findings of the bryostatins, including all the topics involved, from marine biology to medicinal chemistry.

TL;DR: In tests with various human cancer xenograft models, capecitabine was more efficacious at wider dose ranges than either 5-FU or 5'-DFUR and was significantly less toxic to the intestinal tract than the others in monkeys.

TL;DR: The synthesis and the characterization of new thiosemicarbazones deriving from natural aldehydes by means of 1H NMR, IR, and MS techniques is reported.

TL;DR: Theoretical models to virtual screening and rational design of anticonvulsant compounds based on a topological substructural molecular design (TOSS-MODE) approach are developed and some findings reported in the literature that indicate that it is an important pharamacophore are outlined.

TL;DR: Using microwaves, the reaction time has been brought down from hours to seconds with improved yield as compared to conventional heating, and all compounds showed promising antibacterial activity.

TL;DR: The nature of the interactions between Plasmodium falciparum dihydrofolate reductase and antimalarial antifolates including some of their analogues was investigated by molecular modeling in conjunction with the determination of the inhibition constants.

TL;DR: A model able to well correlate the antimycobacterial activity with the chemical structures of pyrrole derivatives 5-33 has been developed which is potentially helpful in the design of novel and more potent antituberculosis agents.

TL;DR: An effective procedure for the synthesis of 2-deoxy-2-fluoro-sugar nucleotide via Select fluor-mediated electrophilic fluorination of glycals with concurrent nucleophilic addition or chemo-enzymatic transformation has been developed, and the fluorinated sugar nucleotides have been used as probes for glycosyltransferases, including fucosyltransferase III, V, VI, and VII.

TL;DR: The results suggested that 3,5-Bis(3'-indolyl)-2(1H)pyrazinone and 3,6-bis[3'-(N-methyl-indolyL)] pyrazine offer potential as lead compounds for the discovery of anticancer agents.

TL;DR: The search for antibiotic compounds has recently taken on a new urgency because of the world-wide increase in bacterial resistance to current antibiotics, which impacts both hospital and community based programs for previously treatable infections.

TL;DR: It is shown that the dipeptide seryl-histidine (Ser-His) and related oligopeptides can themselves cleave DNA, protein, and the ester p-nitrophenyl acetate (p-NPA) over wide ranges of pH and temperature.

TL;DR: According to the results, the design of molecules with the side chain bound to the ethylene part of the triphenyl ethylene skeleton might generate compounds of potential pharmacological interest.

TL;DR: The design and the synthesis of some aryl-substituted pyrrolizine and indolizine derivatives are reported, on the basis of a hypothetical pharmacophore structure designed to fit the catalytic site of the human cytochrome P450 aromatase.

TL;DR: Circular dichroism (CD) studies suggest that the stereochemistry of the PS-oligo does not affect the global conformation of the duplex, and protein- and enzyme-binding studies showed insignificant stereo-dependent binding to proteins.

TL;DR: Two new aryl azides, modeled after the potent antitumor, antimitotic agent combretastatin A-4 (CA-4), have been prepared by chemical synthesis as potentially useful photoaffinity labeling reagents for the colchicine site on beta-tubulin.

TL;DR: It is derived that the indenoquinoline nucleus probably represents the maximum allowable molecular size for rigid compounds binding to AChE, and seems particularly important in the context of Alzheimer's disease research in the light of recent observations showing that peripheral A ChE inhibitors might decrease the aggregating effects of the enzyme on the beta-amyloid peptide (betaA).

TL;DR: 2'-Malyl pac litaxel sodium salt demonstrated enhanced antitumour activity and less toxicity in a P388 murine leukaemia in vivo model when compared to paclitaxel.

TL;DR: The overall rat behavioral profile of this compound suggests that it may be an anxiolytic drug with a low motor side effect liability.

TL;DR: Results obtained in agar dilution assays have shown that 4-aryl homoallylamines not possessing halogen in their structures, tetrahydroquinolines and quinolines, display a range of antifungal properties in particular against Epidermophyton floccosum and Microsporum canis.

TL;DR: Saturation of the side chain resulted in significantly enhanced inhibition of CYP while modifications in the phenyl and basic moieties in few analogues offered maximal selectivity in inhibiting either constitutive or inducible CYP activities.

TL;DR: All compounds were able to induce direct cytotoxicity only at very high concentrations but showed a remarkable indirect activity and in particular compound 4d was able to significantly increase macrophage lytic properties and has been selected for further investigations.

TL;DR: A series of dimeric compounds linked through the 6-carboxamides were prepared by coupling the requisite acid imidazolides with various diamines, giving growth delays comparable to that of the clinical topo I inhibitor irinotecan at up to 10-fold lower doses.

TL;DR: Results appear to strengthen the role of adducts between art Artemisinin derivatives and heme in generation of artemisinin radicals.

TL;DR: Results suggest that DU-257 will be one of the candidate of anti-tumor agent for application to immunoconjugate and its conjugate with KM231 via PEG-dipeptidyl linker will be a useful entity for cancer therapy related to sLe(a) expression.

TL;DR: Highly regioselective electrophilic substitution of dibenzofluorene was achieved and the nitro derivative was transformed to a variety of new anticancer agents.

TL;DR: The synthesis of new imidazo[2,1-b]thiazole guanylhydrazones which were tested as potential antitumor agents and three of these derivatives were the most potent and one of these showed a mild effect as CDK1 inhibitor.

TL;DR: It is demonstrated that removal of the N atom from a typical phenylalkylpiperidine led to little or no binding to sigma receptors, and where two N atoms occur in a compound, such as with phenylalkylpiperazines, the N atoms on the longer alkyl chain appears to be more important.

TL;DR: In order to gain an insight into the structural principles governing subtype selectivity, ligand based drug design methods have been used to design a novel 1,2,3-thiadiazole ring d analogue of the aporphine system.