1,721,091 research outputs found
Synthesis 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
Synthesis and SIRT1 modulation studies of amides and hydrazides of benzoic acid incorporating a (2-trifluoromethylpyridin-4-yl)amino moiety
No full textSynthesis and in vitro antitumoral activity of new N-phenyl-3-pyrrolecarbothioamides
No full textA new series of N-phenylpyrrolecarbothioamides were obtained from base catalyzed intramolecular cyclization of 3-amino-3-(alkyl or arylamino)propenethioamides. Pyrrole derivatives were evaluated for their in vitro anticancer activity toward cell lines of nine different types of human cancer. Some of newly prepared compounds demonstrated inhibitory effects on the growth of a wide range of cancer cell lines generally at 10−6 M level and in some case at 10−8 M concentrations
17) Derivati propenetioamidici quali precursori sintetici di eterociclici biologicamente attivi
No full textNew potential imidazole-based antitumor agents. Synthesis and antiproliferative activity
No full textSynthesis 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
Synthesis of 1-acyl-5-pyrazolones and pyrrolidino [2,3-c]pyrazol-3-ones
No full textThe reactivity of acetamidrazones I in strong basicity conditions was examined. When compounds I are reacted with equivalent quantities of α-haloketones in sodium alcoholate, the pyrrolidino[2,3-c]pyrazol-3-ones IV were obtained by intermediate formation of 1-acyl-3-amino-5-pyrazolones III
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
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