2. Academic Validation
  3. Synthesis and anticancer activity of some pyrimidine derivatives with aryl urea moieties as apoptosis-inducing agents

Synthesis and anticancer activity of some pyrimidine derivatives with aryl urea moieties as apoptosis-inducing agents

  • Bioorg Chem. 2020 Aug;101:104028. doi: 10.1016/j.bioorg.2020.104028.
Zühal Kilic-Kurt 1,  Nuri Ozmen 2,  Filiz Bakar-Ates 2
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Ankara, Turkey. Electronic address: zkurt@ankara.edu.tr.
  • 2 Department of Biochemistry, Faculty of Pharmacy, Ankara University, Ankara, Turkey.
PMID: 32645482 DOI: 10.1016/j.bioorg.2020.104028
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.

Keywords

Anticancer; Apoptosis mechanism; Pyrimidines; Synthesis; Urea.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z