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
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概要
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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 µM 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 µM.
著者
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Ruiz Ana
Centro Nacional De Microelectronica:(present Address) Instituto De Ciencia De Materiales
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Da Silva
Departamento De Biologia Celular Universidade De Brasilia
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Da Costa
Departamento De Biologia Centro De Ciencias Universidade Federal Do Ceara
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Leite Silva
Departamento de Química, Universidade Estadual de Maringá
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Garcia Francielle
Departamento de Ciências Básicas da Saúde, Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Bloco B-08 Sala 06 CCS, Universidade Estadual de Maringá
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Rodrigues Jean
Departamento de Ciências Básicas da Saúde, Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Bloco B-08 Sala 06 CCS, Universidade Estadual de Maringá
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Nakamura Celso
Departamento de Ciências Básicas da Saúde, Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Bloco B-08 Sala 06 CCS, Universidade Estadual de Maringá
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Ueda-Nakamura Tania
Departamento de Ciências Básicas da Saúde, Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Bloco B-08 Sala 06 CCS, Universidade Estadual de Maringá
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Meyer Emerson
Departamento de Química, Universidade Estadual de Maringá
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Foglio Mary
Centro Pluridisciplinar de Pesquisas Químicas, Biológicas e Agrícolas (CPQBA), Universidade Estadual de Campinas
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de Carvalho
Centro Pluridisciplinar de Pesquisas Químicas, Biológicas e Agrícolas (CPQBA), Universidade Estadual de Campinas
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Sarragiotto Maria
Departamento de Química, Universidade Estadual de Maringá
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Garcia Francielle
Departamento de Ciências Básicas da Saúde, Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Bloco B-08 Sala 06 CCS, Universidade Estadual de Maringá
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de Carvalho
Centro Pluridisciplinar de Pesquisas Químicas, Biológicas e Agrícolas (CPQBA), Universidade Estadual de Campinas
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da Costa
Departamento de Química, Universidade Estadual de Maringá
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Foglio Mary
Centro Pluridisciplinar de Pesquisas Químicas, Biológicas e Agrícolas (CPQBA), Universidade Estadual de Campinas
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Meyer Emerson
Departamento de Química, Universidade Estadual de Maringá
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Silva Camila
Departamento de Química, Universidade Estadual de Maringá
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Leite Silva
Departamento de Química, Universidade Estadual de Maringá
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Rodrigues Jean
Departamento de Ciências Básicas da Saúde, Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Bloco B-08 Sala 06 CCS, Universidade Estadual de Maringá
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Ueda-Nakamura Tania
Departamento de Ciências Básicas da Saúde, Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Bloco B-08 Sala 06 CCS, Universidade Estadual de Maringá
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Sarragiotto Maria
Departamento de Química, Universidade Estadual de Maringá
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Nakamura Celso
Departamento de Ciências Básicas da Saúde, Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Bloco B-08 Sala 06 CCS, Universidade Estadual de Maringá
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