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Synthesis and activity evaluation of PARP-1 inhibitors with azaindole skeleton / 药学学报
Acta Pharmaceutica Sinica ; (12): 1792-1799, 2013.
Artigo em Chinês | WPRIM | ID: wpr-298009
ABSTRACT
PARP [poly(ADP-ribose)polymerase] represents a novel potential target in cancer therapy. It is involved in a DNA repair process by catalyzing the transfer of ADP-ribose units from NAD to a number of its substrate proteins. In this work, a series of novel azaindole derivatives was designed and synthesized. Moreover, 16 target molecules were screened and 8 compounds displayed inhibitory activity against PARP-1. It has been demonstrated that these azaindoles bearing cycloamine substituents at 2-position were active to both PARP-1 and PARP-2.
Assuntos
Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Farmacologia / Compostos Aza / Química / Poli(ADP-Ribose) Polimerases / Poli(ADP-Ribose) Polimerase-1 / Indóis / Metabolismo / Antineoplásicos Idioma: Chinês Revista: Acta Pharmaceutica Sinica Ano de publicação: 2013 Tipo de documento: Artigo

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Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Farmacologia / Compostos Aza / Química / Poli(ADP-Ribose) Polimerases / Poli(ADP-Ribose) Polimerase-1 / Indóis / Metabolismo / Antineoplásicos Idioma: Chinês Revista: Acta Pharmaceutica Sinica Ano de publicação: 2013 Tipo de documento: Artigo