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Type: Artigo de periódico
Title: Synthesis, Antitumor, Antitrypanosomal and Antileishmanial Activities of Benzo[4,5]canthin-6-ones Bearing the N '-(Substituted benzylidene)-carbohydrazide and N-Alkylcarboxamide Groups at C-2
Author: Silva, CMBL
Garcia, FP
Rodrigues, JHD
Nakamura, CV
Ueda-Nakamura, T
Meyer, E
Ruiz, ALTG
Foglio, MA
de Carvalho, JE
da Costa, WF
Sarragiotto, MH
Abstract: A series of novel benzo[4,5]canthin-6-ones, bearing the N'-(substituted benzylidene)-carbohydrazide (11a-e) and N-alkylcarboxamide (13a-g) moieties at position-2, were synthesized and screened for their in vitro antitumor activity, against seven human cancer cell lines, and for antitrypanosomal and antileishmanial activities against Trypanosoma cruzi and Leishmania amazonensis. The results indicated that N-methylpiperazyl-6-oxobenzo[4,5]canthine-2-carboxamide (13f) displayed potent antitumor activity with IC50 values in the range of 1.15-8.46 mu m for all cell lines tested. Compounds 13f and 13g bearing an N-methylpiperazylcarboxamide and N-morpholylcarboxamide at C-2, respectively, showed potent activities towards both Trypanosoma cruzi and Leishmania amazonensis parasites, with IC50, in the range of 0.4 to 16.70 mu m.
Subject: benzocanthinone
antitumor activity
antitrypanosomal activity
antileishmanial activity
Country: Japão
Editor: Pharmaceutical Soc Japan
Citation: Chemical & Pharmaceutical Bulletin. Pharmaceutical Soc Japan, v. 60, n. 11, n. 1372, n. 1379, 2012.
Rights: aberto
Date Issue: 2012
Appears in Collections:Unicamp - Artigos e Outros Documentos

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