期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 20, 期 4, 页码 1417-1424出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.01.003
关键词
p53-MDM2 binding inhibitors; 2,4,5-Triphenyl imidazoline; Anti-proliferative activities; CoMFA
资金
- National Natural Science Foundation of China [30873163]
- Scholarship Award for Excellent Doctoral Student
- Ministry of Education
- Zhejiang Innovation Program for Graduates [YK2010012]
A series of novel N1-amino-acid substituted 2,4,5-triphenyl imidazoline derivatives was designed and synthesized based on our previous studies. All synthesized target compounds were screened for their p53-MDM2 binding inhibitory activities and anti-proliferative activities against five cancer cell lines. Among them, twelve compounds displayed improved binding inhibitory activities and most compounds showed higher cell growth inhibition activities with IC50 values in the low micromolar range. Compound 6c exhibited marked p53-MDM2 binding inhibitory activity (IC50 = 0.59 mu M) which was eightfold more potent than that of Nutlin-1 (IC50 = 4.78 mu M). CoMFA analysis was performed based on obtained biological data and resulted in a statistically significant CoMFA model with high predict abilities (q(2) = 0.645, r(2) = 0.979). (C) 2012 Elsevier Ltd. All rights reserved.
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