Synthesis and Antitumoral Evaluation of Benzyl (1S)-2-[2-(monosubstituted-benzylidene)hydrazino]-1-(hydroxymethyl)-2-oxoethylcarbamate

Letters in Drug Design & Discovery(2012)

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摘要
A series of 14 N-acyl-hydrazones L-serine derivatives have been synthesized and evaluated for their in vitro antitumoral activities against four neoplastic cancer cells: HL-60 (leukemia), MDA-MB-435 (melanoma), HCT-8 (colon) and SF-295 (nervous system). Five compounds (3g, 3h, 3i, 3k and 3n) were considered active against at least two cancer cell lines, with more than 90% of growth inhibition. Compound 3h, with IC50 of 2.04 mu g/mL, seems to be moderately selective to HCT-8 and can be considered in further studies aiming new prototypes for a lead molecule against colon cancer.
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关键词
Hydrazones,L-serine,Cancer,Conagenin,Lymphokines
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