Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


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

Author(s): Raquel Carvalho Montenegro, Leticia Veras Costa Lotufo, Manoel Odorico de Moraes, Claudia do O Pessoa, Felipe Augusto Rocha Rodrigues, Alessandra Campbell Pinheiro, Thais Cristina Mendonça Nogueira, Marcus Vinicius Nora de Souza.


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 μg/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.

Keywords: L-serine, Hydrazones, Cancer, Conagenin, Lymphokines, Antitumoral Evaluation, Streptomyces roseosporus, ceramidase inhibitors, apoptosis, tumor suppressor lipid, sphingosine kinase inhibitor, Pharmacological Studies, Melting points, IC50

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Article Details

Year: 2012
Page: [257 - 262]
Pages: 6
DOI: 10.2174/157018012799129800
Price: $58