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

Authors: Montenegro, R.C.; Lotufo, L.V.; Moraes, M.O.; Pessoa, C.O.; Rodrigues, F.A.R.; Pinheiro, A.C.; Nogueira, T.C.M.; De Souza, M.V.N.


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. – See more at: http://www.eurekaselect.com/89481/article#sthash.4B5LH58q.dpuf

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 – See more at: http://www.eurekaselect.com/89481/article#sthash.4B5LH58q.dpuf Document Type: Research Article DOI: http://dx.doi.org/10.2174/157018012799129800 Publication date: 1 de Janeiro de 2012

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