Synthesis and Antiproliferative Activitiy of Novel Diaryl Ureas Possessing a 4H-Pyrido[1,2-a]pyrimidin-4-one Group

Synthesis and Antiproliferative Activitiy of Novel Diaryl Ureas Possessing a 4H-Pyrido[1,2-a]pyrimidin-4-one Group
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具有4H-吡啶并[1,2-a]嘧啶-4-酮基团的新型二芳基脲的合成及其抗增殖活性

DOI:
10.1002/ardp.200900130
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发表时间:
2010-01-01
影响因子:
5.1
通讯作者:
Gong, Ping
Gong, Ping
中科院分区:
医学3区
文献类型:
--
作者:
Yao, Peng;Zhai, Xin;Gong, Ping

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We herein disclose a series of novel diaiyl urea derivatives possessing a 4H-pyrido[1,2-a]pyrimidin-4-one group as novel potent anticancer compounds. The structures were confirmed by IR, H-1-NMR, and MS. All the compounds were screened for their antiprofilerative activity agaist 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 (IC50 = 0.7 mu mol/L), with a potency 3.6-fold higher than Sorafenib (IC50 = 2.5 mu mol/L), which was approved in 2005.