1,721,142 research outputs found
Special Issue “Novel Anti-Proliferative Agents”
Full text linkCancer is a disease that can affect any organ and spread to other nearby or distant organs [...
Dual action inhibitors of endocannabinoid metabolism and prostaglandin formation as novel analgesics
No full textSynthesis and biological evaluation of novel acylhydrazone derivatives as potential antitumor agents
No full textWe have designed, synthesized, and evaluated as potential antitumor agents a series of 2-hydroxybenzylidene derivatives of the N-(2-trifluoromethylpiridyn-4-yl)anthranilic acid hydrazide, and some analogues bearing a (2-trifluoromethyl)piridyn-4-ylamino group in 3- or 4- position of benzohydrazide or 4- position of phenylacetohydrazide. Compounds 12e, 13e, 15e, and 16e, bearing a 4-(diethylamino)salicylidene group exhibited potent cytotoxicity, with averaged GI50 values in sub-micromolar range, and a variety of cell selectivity at nanomolar concentrations. The determination of acute toxicity in athymic nudes mice proved some compounds to be non-toxic, making them good candidates for further study as antitumor agents
AN IMPROVED PROCEDURE FOR THE PREPARATION OF SUBSTITUTED THIAZOLES
No full textThe reaction between 3-amino-3-(dialkylamino)propenenitriles 1 and sodium thiocyanate in presence of bromine, provides an efficient route for the synthesis of 2-amino-5-cyano-4-(dialkylamino)thiazoles 3
Synthesis and structural studies of 3-acylamino-4-amino-2,3-dihydro-2-iminothiazole-5-carboxylates and 4-acylhydrazino-2-aminothiazole-5-carboxylates
No full textThe preparation of thiazole derivatives through reactions of ethyl 3-amino-3-acylhydrazinopropenoates (1) with inorganic thiocyanates and thiourea was investigated. The reaction of 1 with sodium thiocyanate, in acetic acid in the presence of bromine, afforded ethyl 3-acylamino-4-amino-2,3-dihydro-2-iminothiazole-5-carboxylates (3) selectively. On reacting the same compounds (1) with thiourea, in acetic acid and in the presence of bromine, 4-acylhydrazino-2-aminothiazole-5-carboxylates (4) were yielded. The structure of the representative compound (3c), ethyl 4-amino-3-benzoylamino-2,3-dihydro-2-iminothiazole-5-carboxylate has been solved by means of X-Ray crystallographic data analysis
Propenethioamides in the synthesis of heterocyclic systems. Synthesis of pyrrole and 1,4-thiazepine derivatives
No full textThe reaction of propenethioamides 1 with bromoketones 2 and 3 led in acidic medium to the formation of 1,4-thiazepines 6 and 7. The pyrrole derivatives 4 and 5 were obtained by reaction of 1 with 2 and 3 in basic medium
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues
No full textA series of new 1,4-diarylimidazol-2(3H)-one derivatives and their 2-thione analogues has been prepared and evaluated
in vitro for antitumor activity against the NCI human cancer cell panel. Compounds bearing a 3,4,5-trimethoxyphenyl ring linked to
either N-1 or C-4 position of the imidazole core demonstrated an interesting profile of cytotoxicity with preferential activity against
leukemic cell lines. Compound 13 exhibited a potent antitumor activity against MOLT-4 (GI50 = 20 nM) and SR (GI50 = 32 nM)
cell lines
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