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Molecular diversity of phenothiazines: design and synthesis of phenothiazine-dithiocarbamate hybrids as potential cell cycle blockers.
Mol Divers; 21(4): 933-942, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28785928
ABSTRACT
Novel phenothiazine-dithiocarbamate analogues were designed by molecular hybridization strategy and synthesized and evaluated for their anticancer activity in vitro against three selected cancer cell lines (EC-109, MGC-803, and PC-3). The preliminary structure-activity relationship (SAR) for this phenothiazine-dithiocarbamate hybrids is explored. Among all analogues, 2-oxo-2-(10H-phenothiazin-10-yl)ethyl 4-ethylpiperazine-1-carbodithioate (8a) showed the most potent inhibitory activity with an [Formula: see text] value of [Formula: see text] against PC-3 cells. In addition, compound 8a could arrest the cell cycle at the G1 phase and regulate the expression of G1 checkpoint-related proteins, suggesting that phenothiazine-dithiocarbamate hybrids might be useful as cell cycle blockers.
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Texto completo: Disponível Coleções: Bases de dados internacionais Base de dados: MEDLINE Assunto principal: Fenotiazinas / Desenho de Drogas / Pontos de Checagem do Ciclo Celular / Antineoplásicos Limite: Humanos Idioma: Inglês Revista: Mol Divers Assunto da revista: Biologia Molecular Ano de publicação: 2017 Tipo de documento: Artigo País de afiliação: China