源自SU5416的康普瑞他汀A-4构象受限类似物的构效关系研究
Structure-activity-relationship studies of conformationally restricted analogs of combretastatin A-4 derived from SU5416.
作者信息
Pandit Bulbul, Sun Yanjun, Chen Ping, Sackett Dan L, Hu Zhigen, Rich Wendy, Li Chenglong, Lewis Andrew, Schaefer Kevin, Li Pui-Kai
机构信息
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
出版信息
Bioorg Med Chem. 2006 Oct 1;14(19):6492-501. doi: 10.1016/j.bmc.2006.06.017. Epub 2006 Jul 24.
A series of combretastatin A-4 analogs derived from the ATP competitive, VEGF receptor tyrosine kinase inhibitor, SU5416 were synthesized. The cytotoxic effects of the analogs were evaluated against PC-3 and MDA-MB-231 cancer cell lines, as well as their abilities to inhibit tubulin polymerization. Results are compared to those of compound 1, our lead compound previously reported.
合成了一系列源自ATP竞争性血管内皮生长因子受体酪氨酸激酶抑制剂SU5416的康普瑞他汀A-4类似物。评估了这些类似物对PC-3和MDA-MB-231癌细胞系的细胞毒性作用，以及它们抑制微管蛋白聚合的能力。将结果与我们之前报道的先导化合物化合物1的结果进行了比较。
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