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Type: Artigo de periódico
Title: Synthesis And Antitumor Activity Of β-carboline 3-(substituted- Carbohydrazide) Derivatives
Author: Barbosa V.A.
Formagio A.S.N.
Savariz F.C.
Foglio M.A.
Spindola H.M.
De Carvalho J.E.
Meyer E.
Sarragiotto M.H.
Abstract: A series of β-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 b-carboline N-(substituted-benzylidene)carbohydrazides showed, in general, a greater antitumor activity than their N-(alkylidene)carbohydrazide analogues. The N 9-methylation of b-carboline N-(substituted-benzylidene) carbohydrazides resulted in a decrease of antitumor activity. Among compounds tested, the benzylidenecarbohydrazides 3, 4, 11, 13, 16, 21 and 22 were the most active, possessing IC 50 less than 10 μMfor 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 (IC 50 = 0.04 lM). Compound 4 was assayed for its in vivo antineoplastic activity in the Ehrlich solid carcinoma assay. © 2011 Elsevier Ltd. All rights reserved.
Rights: fechado
Identifier DOI: 10.1016/j.bmc.2011.08.059
Date Issue: 2011
Appears in Collections:Unicamp - Artigos e Outros Documentos

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