Design, Synthesis and Evaluation of Novel Rhodanine‐containing Sorafenib Analogs as Potential Antitumor Agents
Design, Synthesis and Evaluation of Novel Rhodanine‐containing Sorafenib Analogs as Potential Antitumor Agents
复制标题
DOI：
10.1002/ardp.201000326
复制
发表时间：
2011-06
影响因子：
5.1
通讯作者：
Wei Li;X. Zhai;Zheng Zhong;Guangyue Li;Yongxiao Pu;P. Gong
中科院分区：
文献类型：
--
作者：
Wei Li;X. Zhai;Zheng Zhong;Guangyue Li;Yongxiao Pu;P. Gong
设计、合成了一系列含罗丹宁的索拉非尼类似物，并评价了它们对三种癌细胞(A549、H460和HT29)的体外抗肿瘤活性。药理实验表明，部分目标化合物的抗增殖活性明显优于参比药物索拉非尼，尤其是最有希望的化合物7R(对A549、H460和HT29细胞的IC50值分别为0.8、1.3和2.8µM)。该活性强烈依赖于C-5“位的罗丹宁基序的取代方式。结果表明，该系列化合物可作为开发新型抗肿瘤药物的基础。
A series of rhodanine‐containing sorafenib analogs was designed, synthesized and evaluated for their in‐vitro antitumor activity against three cancer cell lines (A549, H460 and HT29). Pharmacological data indicated that some of the target compounds possessed marked antiproliferative activity superior to the reference drug sorafenib, especially the most promising compound 7r (with the IC50 value of 0.8, 1.3 and 2.8 µM against A549, H460 and HT29 cell lines, respectively). The activity was found to strongly depend on the substitution pattern of the rhodanine motif at C‐5″ position. Results suggested that this series of compounds could serve as the bases for the development of novel antitumor agents.