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

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

Volume: 9 Issue: 3

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 and Marcus Vinicius Nora de Souza

Affiliation:

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

Abstract: 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.

Cite this article as:

Carvalho Montenegro Raquel, Veras Costa Lotufo Leticia, Odorico de Moraes Manoel, do O Pessoa Claudia, Augusto Rocha Rodrigues Felipe, Campbell Pinheiro Alessandra, Cristina Mendonça Nogueira Thais and Vinicius Nora de Souza Marcus, Synthesis and Antitumoral Evaluation of Benzyl (1S)-2-[2-(monosubstituted-benzylidene)hydrazino]-1-(hydroxymethyl)-2-oxoethylcarbamate, Letters in Drug Design & Discovery 2012; 9 (3) . https://dx.doi.org/10.2174/157018012799129800