Design, Synthesis, and Preliminary Cytotoxicity Evaluation of New Diarylureas and Diarylamides Possessing 1,3,4-Triarylpyrazole Scaffold

Bulletin of the Korean chemical society

Jun Hee Hong¹  Won-Kyoung Choi¹  Hong Seok Choi¹  Daejin Baek¹  Kihang Choi¹  Mohammed I. El-Gamal¹  Chang-Hyun Oh¹ 

关键词: A375P;    Anticancer;    Diarylamide;    Diarylurea;    1;    3;    4-Triarylpyrazole;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

A series of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was synthesized and their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 9, 11, 12, 14, and 17-21 showed superior potency against A375P to Sorafenib. Over the NCI-60 cancer cell line panel, compound 14 possessing a methoxy group, amide linker, and 4-chloro-3- (trifluoromethyl)phenyl terminal ring showed the highest potency and broad-spectrum anticancer activity. Compound 13 showed high selectivity towards leukemia subpanel over other cancer types.

【 授权许可】

Unknown