Artículos de revistas
Synthesis and antitumor activity of beta-carboline 3-(substituted-carbohydrazide) derivatives
Registro en:
Bioorganic & Medicinal Chemistry. Pergamon-elsevier Science Ltd, v. 19, n. 21, n. 6400, n. 6408, 2011.
0968-0896
WOS:000296234900025
10.1016/j.bmc.2011.08.059
Autor
Barbosa, VA
Formagio, ASN
Savariz, FC
Foglio, MA
Spindola, HM
de Carvalho, JE
Meyer, E
Sarragiotto, MH
Institución
Resumen
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) A series of beta-carboline derivatives bearing a substituted-carbohydrazide moiety at C-3 were synthesized and evaluated for their antitumor activity against eight human cancer cell lines. The beta-carboline N-(substituted-benzylidene)carbohydrazides showed, in general, a greater antitumor activity than their N-(alkylidene)carbohydrazide analogues. The N-9-methylation of beta-carboline N-(substituted-benzylidene) carbohydrazides resulted in a decrease of antitumor activity. Among compounds tested, the benzylidene-carbohydrazides 3, 4, 11, 13, 16, 21 and 22 were the most active, possessing IC50 less than 10 mu M for six of the eight tumor cell lines assayed. The derivative 4 displayed the most significant activity toward all tested cell lines, with a remarkable cytotoxicity against renal (786-0) cell lines (IC50 = 0.04 mu M). Compound 4 was assayed for its in vivo antineoplastic activity in the Ehrlich solid carcinoma assay. (C) 2011 Elsevier Ltd. All rights reserved. 19 21 6400 6408 Fundacao Araucaria (Brazil, PR) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Fundacao Araucaria Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)