Showing papers in "Bioorganic & Medicinal Chemistry in 2002"

TL;DR: A survey of representative literature procedures for the preparation of 5-substituted-1H-tetrazoles, focusing on preparations from aryl and alkyl nitriles, is presented in sections by generalized synthetic methods.

TL;DR: A hydrophobic substituent on one aromatic ring, and a hydrogen-bonding group on the other aromatic ring resulted in increased anti-TB activity of the chalcones and chalcone-like compounds.

TL;DR: Results support a role of Mg(2+) ion binding in the selective cytotoxicity of UK-1 and provide a minimal pharmacophore for the select cytotoxic activity of the natural product.

TL;DR: This review focuses on recent advances in the de novo design of nucleoside analogues with improved binding properties and tries to summarize scope and limitations of this design principle.

TL;DR: In this review, a number of synthetic strategies for the generation of benzoannelated nitrogen heterocycles using resin-bound substrates have been described and particular emphasis has been focused on the synthesis of libraries and the use of combinatorial chemistry techniques.

TL;DR: Further studies on the activities of this glycoprotein fraction indicate that a fucose containing polysaccharide fraction is responsible for stimulating the expression of cytokines, especially IL-1, IL-2 and INF-gamma.

TL;DR: Two new series of 2,5-disubstituted-1,3,4-thiadiazoles were synthesized for their possible anticonvulsant, antibacterial and antifungal activities and showed maximum protection against pentylenetetrazole-induced convulsions in mice.

TL;DR: It was found that the substitution pattern on the 5-benzylidene moiety markedly influenced the activity of N-unsubstituted 2,4-thiazolidinediones 2, compounds with substituents at the meta position being generally more effective than the para-subst ituted ones; however, this SAR was not evidenced in acetates 3 and acids 4.

TL;DR: The first published synthesis and characterization of a purine-scaffold library of hsp90 inhibitors is presented and represents a platform for the creation of easily synthesizable and derivatizable soluble molecules that are amenable for oral administration.

TL;DR: The in vitro antitumor activity of the novel compounds was screened and the highest inhibition of tree tumor cell lines was observed for the compounds containing phenylethylenamino and phenylethylamino groups at position 4 of 1,2,4-triazol ring.

TL;DR: New 2-substituted-phenyl-1H-benzimidazole-5-carboxylic acids, and cyano substituted compounds 53, 57, 58 and 61 exhibited the greatest activity with MIC values similar to that of fluconazole.

TL;DR: Salacinol showed potent inhibitory activities on several alpha-glucosidases, such as maltase, sucrase, and isomaltases, and the inhibitory effects on serum glucose levels in maltose- and sucrose-loaded rats (in vivo) were found to be more potent than that of acarbose, a commercial alpha- GLUCosidase inhibitor.

TL;DR: In these series, compound 3e (LASSBio 468), having a sulfonyl-thiomorpholine moiety, showed potent inhibitory activity on LPS-induced neutrophil recruitment with ED(50)=2.5mg kg(-1), which was correlated with its inhibitory effect on TNF-alpha level.

TL;DR: 3,5-dibenzoyl-4-(3-chlorophenyl)-1,4-dihydro-2,6-dimethylpyridine can be recommended as a new drug candidate for MDR cancer treatment.

TL;DR: Several flavonoids, that is apigenin, luteolin, diosmetin, fisetin, and quercet in, inhibited the antigen-IgE-mediated TNF-alpha and IL-4 production from RBL-2H3 cells, both of which participate in the late phase of type I allergic reactions.

TL;DR: Two collections of the marine cyanobacterium Lyngbya sp.

TL;DR: Differences on their potency towards the effect on the growth of the human cancer cell lines as well as on the proliferation of human T-lymphocytes can be ascribed to the nature and positions of the substituents on the xanthonic nucleus.

TL;DR: Curcumin compound was the most potent analogue against several cell lines, including HOS and 1A9 (breast cancer), with ED50 values of 0.97 and <0.63 microg/mL, respectively.

TL;DR: Caffeic acid phenethyl ester and its twenty analogues possessed selective antiproliferative activity toward highly liver-metastatic murine colon 26-L5 carcinoma cell line.

TL;DR: Current knowledge of the structure and function of histidine kinase and the development of antibiotics with a new mode of action are summarized: targeting histidine Kinase promoted signal transduction and its subsequent regulation of gene expression system are summarized.

TL;DR: A series of Taxol derivatives tethered at C2' and C-7 to glutamate and folate have been synthesized for evaluation as prodrugs which release Taxol via hydrolytic lability of their alpha-alkoxy and alpha-amino esters as mentioned in this paper.

TL;DR: Investigation on the structure--antioxidative activity relationships of derivatives of derivatives based on garcinoic acid from Garcinia kola led to discovery of a powerful antioxidative agent.

TL;DR: A series of 4-quinolylhydrazones synthesized and tested against Mycobacterium tuberculosis H37Rv showed interesting antitubercular properties; two compounds (3(2) and 3(25)), identified as the most active, were tested also against MyCobacteria avium.

TL;DR: The cellular uptake and localization properties of DNA binding N-methylpyrrole/N-methylimidazole polyamide-dye conjugates in a variety of living cells have been examined by confocal laser scanning microscopy.

TL;DR: It has been revealed that thalidomide elicits pleiotropic effects and is a multi-target drug.

TL;DR: The reaction of Appel's salt with o-amino nitrile heterocycles 10-19 gave the corresponding 4-chloro-5-heteroimmine-1,2,3-dithiazoles 20-29 which were evaluated for their antibacterial, antifungal and antitumor activity.

TL;DR: A new series of HIV integrase inhibitors, thalassiolins A-C (1-3), isolated from the Caribbean sea grass Thalassia testudinum are described, indicating a favorable binding mode is probable at the catalytic core domain of HIV-1 integrase.

TL;DR: The QSAR model so established here was based on the elucidation of the complex molecular mechanisms, and may reasonably predict the antioxidant activity using simple experimental and calculated parameters.

TL;DR: The methanolic extract from the flowers of Tilia argentea (linden) was found to show a hepatoprotective effect against D-galactosamine (D-GalN)/lipopolysaccharide (LPS)-induced liver injury in mice, and its effect was suggested to depend on the inhibition of tumor necrosis factor-alpha (TNF-alpha) production, decreased sensitivity of hepatocytes to TNF- alpha, and on the protection of hepat

TL;DR: Interestingly, Psammaplin A was found to moderately inhibit chitinase B from Serratia marcescens, the mode of inhibition being non-competitive.