4,5-Diaryl-3-aminopyrazole Derivatives as Analogs of Combretastatin A-4: Synthesis and Biological Evaluation

被引：19
作者：
Liu, Tao [1 ]
Cui, Rong [1 ,2 ]
Chen, Jing [1 ]
Zhang, Jun [3 ]
He, Qiaojun [3 ]
Yang, Bo [3 ]
Hu, Yongzhou [1 ]
机构：
[1] Zhejiang Univ, Coll Pharmaceut Sci, ZJU ENS Joint Lab Med Chem, Hangzhou 310058, Zhejiang, Peoples R China
[2] JinHua Coll Vocat & Technol, Jinhua, Peoples R China
[3] Zhejiang Univ, Coll Pharmaceut Sci, Inst Pharmacol & Toxicol, Hangzhou 310058, Zhejiang, Peoples R China
来源：
ARCHIV DER PHARMAZIE | 2011年 / 344卷 / 05期
关键词：
Antitumor agents; Combretastatin A-4 analogs; Cytotoxicity; 4,5-Diaryl-3-aminopyrazole derivatives; CIS-RESTRICTED ANALOGS; ANTITUMOR AGENTS; ANTINEOPLASTIC AGENTS; TUBULIN; COLCHICINE; DESIGN; INHIBITORS; BINDING; GROWTH;
D O I：
10.1002/ardp.201000069
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of cis-restricted 4,5-diaryl-3-aminopyrazole derivatives were synthesized and tested for their cytotoxic activity in vitro against five human cancer cell lines (K562, ECA-109, A549, SMMC-7721, and PC-3). Compounds 5a, 5b, 5d, and 6b showed potent cytotoxicity against all tested cell lines. Primary mechanism research on compound 5a indicated that it was a potent inhibitor of tubulin polymerization, arresting cell cycle in G(2)/M phase. The docking research showed the conformation of 5a overlaps well with CA-4 in the crystallized protein complex, suggesting the 4,5-diaryl-3-aminopyrazoles were good mimics of CA-4.
引用
收藏
页码：279 / 286
页数：8
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