Synthesis and in vitro antitumor activity of novel diaryl urea derivatives
Synthesis and in vitro antitumor activity of novel diaryl urea derivatives
复制标题
新型二芳基脲衍生物的合成及其体外抗肿瘤活性
DOI：
10.1016/j.cclet.2013.02.004
复制
发表时间：
2013-05-01
影响因子：
9.1
通讯作者：
Gong, Ping
中科院分区：
文献类型：
--
作者：
Zhao, Yan-Fang;Liu, Zi-Jian;Gong, Ping
合成了一系列含有 4-[(2-氨基-6-三氟甲基)嘧啶-4-基]哌嗪-1-基的新型二芳基脲，并评估了它们在一组人类癌细胞系中的细胞毒性活性。与参比药物索拉非尼相比，一些化合物表现出更有效、更广谱的抗癌活性。其中，化合物2p对MDA-MB-231、HT-29和MCF-7细胞系具有显着的抑制活性，IC50值分别为0.016、0.63、0.001 μmol/L。 (C) 2013 乒乓球。由Elsevier B.V.代表中国化学会出版。版权所有。
A series of novel diaryl ureas containing 4-[(2-amino-6-trifluromethyl)pyrimidine-4-yl]piperazine-1-yl group were synthesized and evaluated for their cytotoxic activities in a panel of human cancer cell lines. Compared with the reference drug Sorafenib, some compounds showed more potent and a broader spectrum of anti-cancer activities. Among them, compound 2p demonstrated significant inhibitory activities against MDA-MB-231, HT-29 and MCF-7 cell lines with IC50 values of 0.016, 0.63, 0.001 mu mol/L, respectively. (C) 2013 Ping Gong. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.