Synthesis and biological evaluation of 3,4-diaryl-5-aminoisoxazole derivatives

被引：41

作者：

Liu, Tao ^{[1
]}

Dong, Xiaowu ^{[1
]}

Xue, Na ^{[1
]}

Wu, Rui ^{[2
]}

He, Qiaojun ^{[2
]}

Yang, Bo ^{[2
]}

Hu, Yongzhou ^{[1
]}

机构：

[1] Zhejiang Univ, Coll Pharmaceut Sci, ZJU ENS Joint Lab Med Chem, Hangzhou 310058, Zhejiang, Peoples R China

[2] Zhejiang Univ, Coll Pharmaceut Sci, Inst Pharmacol & Toxicol, Hangzhou 310058, Zhejiang, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 17期

关键词：

3,4-Diaryl-5-aminoisoxazole; Cytotoxic activities; Tubulin polymerization inhibition; COMBRETASTATIN A-4 ANALOGS; ANTITUMOR AGENTS; TUBULIN; COLCHICINE; CHEMISTRY; BINDING;

D O I：

10.1016/j.bmc.2009.07.040

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of cis-restricted 3,4-diaryl-5-aminoisoxazoles have been synthesized and evaluated for their biological activities. Among them, compound 11a and 13a displayed potent cytotoxic activities in vitro against five human cancer cell lines with IC50 values in the low micromolar range and two compounds inhibited tubulin polymerization with IC50 value of 1.8, and 2.1 mu M, respectively, similar to that of CA-4. Compound 13a could arrest at the G2/M phase of the cell cycle at the concentration of 0.1 and 1.0 mu M and induce apoptosis at 0.1-1.0 mu M. (C) 2009 Elsevier Ltd. All rights reserved.

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收藏

页码：6279 / 6285

页数：7

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