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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

Camila Mareco Bento Leite Silva ; Garcia, Francielle Pelegrin ; Jean Henrique da Silva Rodrigues ; Nakamura, Celso Vataru ; Ueda-Nakamura, Tania ; Meyer, Emerson ; Ana Lucia Tasca Gois Ruiz ; Foglio, Mary Ann ; Carvalho, João Ernesto de ; Costa, Willian Ferreira da ; Sarragiotto, Maria Helena

Chemical and Pharmaceutical Bulletin, 2012/11/01, Vol.60(11), pp.1372-1379 [Periódico revisado por pares]

Japan: The Pharmaceutical Society of Japan

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Título:
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
Autor: Camila Mareco Bento Leite Silva ; Garcia, Francielle Pelegrin ; Jean Henrique da Silva Rodrigues ; Nakamura, Celso Vataru ; Ueda-Nakamura, Tania ; Meyer, Emerson ; Ana Lucia Tasca Gois Ruiz ; Foglio, Mary Ann ; Carvalho, João Ernesto de ; Costa, Willian Ferreira da ; Sarragiotto, Maria Helena
Assuntos: antileishmanial activity ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - pharmacology ; antitrypanosomal activity ; antitumor activity ; benzocanthinone ; Benzylidene Compounds - chemical synthesis ; Benzylidene Compounds - chemistry ; Benzylidene Compounds - pharmacology ; benzylidenecarbohydrazide ; Carbolines ; carboxamide ; Cell Line, Tumor ; Chagas Disease - drug therapy ; Humans ; Indole Alkaloids ; Indoles - chemical synthesis ; Indoles - chemistry ; Indoles - pharmacology ; Inhibitory Concentration 50 ; Leishmania - drug effects ; Leishmaniasis - drug therapy ; Naphthyridines - chemical synthesis ; Naphthyridines - chemistry ; Naphthyridines - pharmacology ; Neoplasms - drug therapy ; Trypanocidal Agents - chemical synthesis ; Trypanocidal Agents - chemistry ; Trypanocidal Agents - pharmacology ; Trypanosoma cruzi - drug effects
É parte de: Chemical and Pharmaceutical Bulletin, 2012/11/01, Vol.60(11), pp.1372-1379
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
Descrição: 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.
Editor: Japan: The Pharmaceutical Society of Japan
Idioma: Inglês;Japonês

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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

Camila Mareco Bento Leite Silva ; Garcia, Francielle Pelegrin ; Jean Henrique da Silva Rodrigues ; Nakamura, Celso Vataru ; Ueda-Nakamura, Tania ; Meyer, Emerson ; Ana Lucia Tasca Gois Ruiz ; Foglio, Mary Ann ; Carvalho, João Ernesto de ; Costa, Willian Ferreira da ; Sarragiotto, Maria Helena

Japan: The Pharmaceutical Society of Japan

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