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

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 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 (IC 50 = 0.7 μmol/L), with a potency 3.6‐fold higher than Sorafenib (IC 50 = 2.5 μmol/L), which was approved in 2005.