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Synthesis and Antiproliferative Activitiy of Novel Diaryl Ureas Possessing a 4 H‐ Pyrido[1,2‐ a ]pyrimidin‐4‐one Group
Author(s) -
Yao Peng,
Zhai Xin,
Liu Dong,
Qi Bao Hui,
Tan Hai Liang,
Jin Yong Cai,
Gong Ping
Publication year - 2010
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200900130
Subject(s) - chemistry , potency , stereochemistry , sorafenib , urea , proton nmr , cancer cell lines , cell culture , human breast , cancer cell , in vitro , cancer , biochemistry , medicine , biology , hepatocellular carcinoma , genetics
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.