Synthesis and Antiproliferative Activitiy of Novel Diaryl Ureas Possessing a 4H‐Pyrido[1,2‐a]pyrimidin‐4‐one Group |
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| Authors: | Peng Yao Xin Zhai Dong Liu Bao Hui Qi Hai Liang Tan Yong Cai Jin Ping Gong |
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| Institution: | Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, P. R. China. Fax: +86 24 2398‐6429 |
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| Abstract: | We herein disclose a series of novel diaryl urea derivatives possessing a 4H‐pyrido1,2‐a]pyrimidin‐4‐one group as novel potent anticancer compounds. The structures were confirmed by IR, 1H‐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 μmol/L), with a potency 3.6‐fold higher than Sorafenib (IC50 = 2.5 μmol/L), which was approved in 2005. |
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| Keywords: | Antiprofilerative activity 4H‐Pyrido[1 2‐a]pyrimidin‐4‐one Synthesis |
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