Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Ping Gong, 103 Wenhua Road, Shenyang, P. R. China.
Arch Pharm (Weinheim). 2010 Jan;343(1):17-23. doi: 10.1002/ardp.200900130.
We herein disclose a series of novel diaryl urea derivatives possessing a 4H-pyrido[1,2-a]pyrimidin-4-one group as novel potent anticancer compounds. The structures were confirmed by IR,(1)H-NMR, and MS. All the compounds were screened for their antiproliferative activity against the human breast cancer cell line (MDA-MB-231). The pharmacological results indicated that most of the compounds showed moderate activity. The best of this series is compound 4c (IC(50)= 0.7 micromol/L), with a potency 3.6-fold higher than Sorafenib (IC(50) = 2.5 micromol/L), which was approved in 2005.
我们在此披露了一系列新型的二芳基脲衍生物，它们具有 4H-吡啶并[1,2-a]嘧啶-4-酮基团，作为新型有效的抗癌化合物。这些结构通过 IR、(1)H-NMR 和 MS 得到了确认。所有化合物都对人乳腺癌细胞系 (MDA-MB-231) 的增殖活性进行了筛选。药理结果表明，大多数化合物表现出中等活性。该系列中最好的是化合物 4c（IC(50)=0.7μmol/L），其活性比索拉非尼（IC(50)=2.5μmol/L）高 3.6 倍，后者于 2005 年获得批准。
