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Synthesis and anticancer activity of some pyrimidine derivatives with aryl urea moieties as apoptosis-inducing agents.
Kilic-Kurt, Zühal; Ozmen, Nuri; Bakar-Ates, Filiz.
Afiliação
  • Kilic-Kurt Z; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Ankara, Turkey. Electronic address: zkurt@ankara.edu.tr.
  • Ozmen N; Department of Biochemistry, Faculty of Pharmacy, Ankara University, Ankara, Turkey.
  • Bakar-Ates F; Department of Biochemistry, Faculty of Pharmacy, Ankara University, Ankara, Turkey.
Bioorg Chem ; 101: 104028, 2020 08.
Article em En | MEDLINE | ID: mdl-32645482
ABSTRACT
A new series of pyrimidine derivatives containing aryl urea moieties was designed and synthesized. The anticancer activities of all compounds were evaluated in vitro against colon and prostat cancer cell lines by MTT assay. Among these compounds, 4b exhibited the highest cytotoxic activity against SW480 cancer cell line with IC50 value of 11.08 µM. Mechanistic studies showed that compound 4b arrested cell cycle at G2/M phase and induced apoptosis through upregulating Bax, Ikb-α and cleaved PARP and downregulating Bcl-2 expression levels. Moreover, compound 4b induced loss of mitochondrial membrane potential in SW480 cells. These results suggest that pyrimidine with urea moieties could be a template for designing new anticancer agents.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Ureia / Apoptose / Antineoplásicos Limite: Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Ureia / Apoptose / Antineoplásicos Limite: Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article