含硫脲的索拉非尼类似物的设计、合成及抗肿瘤活性研究。
Design, synthesis and biological activities of thiourea containing sorafenib analogs as antitumor agents.
机构信息
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan, Shandong 250012, PR China.
出版信息
Bioorg Med Chem. 2012 May 1;20(9):2923-9. doi: 10.1016/j.bmc.2012.03.018. Epub 2012 Mar 14.
A novel series of diaryl thiourea containing sorafenib derivatives 9a-t was designed and synthesized. The structures of all the newly synthesized compounds were determined by (1)H NMR, (13)C NMR and HRMS. Their antiproliferative activities against HCT116 and MDA-MB-231 cell lines, and their inhibitory activities against the phosphorylation of VEGFR were evaluated and described. Some of the compounds showed significant activities against both cell lines and VEGFR. Compounds 9g, 9m, 9o and 9p demonstrated competitive antiproliferative activities to sorafenib, the reference standard, while compounds 9d, 9m, and 9p showed significant inhibitory activities against the phosphorylation of VEGFR.
设计并合成了一系列新型含索拉非尼的二芳基硫脲衍生物 9a-t。所有新合成化合物的结构均通过 1H NMR、13C NMR 和 HRMS 确定。评估并描述了它们对 HCT116 和 MDA-MB-231 细胞系的增殖抑制活性及其对 VEGFR 磷酸化的抑制活性。一些化合物对两种细胞系和 VEGFR 均表现出显著的活性。化合物 9g、9m、9o 和 9p 对索拉非尼（参比标准）表现出竞争性的增殖抑制活性，而化合物 9d、9m 和 9p 对 VEGFR 磷酸化表现出显著的抑制活性。
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