Synthesis and antiproliferative activity of novel diaryl ureas possessing a 4H-pyrido[1,2-a]pyrimidin-4-one group
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Published on: June 23, 2019
1Key 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.
Abstract:
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.
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