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

被引：13
作者：
Choi, Won-Kyoung [1 ,4 ]
El-Gamal, Mohammed I. [1 ,2 ,6 ]
Choi, Hong Seok [3 ]
Hong, Jun Hee [3 ]
Baek, Daejin [5 ]
Choi, Kihang [4 ]
Oh, Chang-Hyun [1 ,2 ]
机构：
[1] Korea Inst Sci & Technol, Ctr Biomat, Seoul 130650, South Korea
[2] Univ Sci & Technol, Dept Bimol Sci, Taejon 305333, South Korea
[3] Chosun Univ, Coll Pharm, Kwangju 501759, South Korea
[4] Korea Univ, Dept Chem, Seoul 136701, South Korea
[5] Hanseo Univ, Dept Chem, Seosan 356706, South Korea
[6] Univ Mansoura, Fac Pharm, Dept Med Chem, Mansoura 35516, Egypt
来源：
BULLETIN OF THE KOREAN CHEMICAL SOCIETY | 2012年 / 33卷 / 09期
关键词：
A375P; Anticancer; Diarylamide; Diarylurea; 1,3,4-Triarylpyrazole; MELANOMA-CELL LINE; ANTIPROLIFERATIVE ACTIVITY; DERIVATIVES; DISCOVERY;
D O I：
10.5012/bkcs.2012.33.9.2991
中图分类号：
O6 [化学];
学科分类号：
0703 ;
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.
引用
收藏
页码：2991 / 2998
页数：8
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