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Synthesis and antiproliferative activity of novel 4-substituted-phenoxy-benzamide derivatives
Authors:Chi-Yu Sun  Yang-Sheng Li  Ai-Long Shi  Ya-Fei Li  Rui-Fang Cao  Huai-Wei Ding  Qing-Qing Yin  Li-Juan Zhang  Hua-Chuan Zheng  Hong-Rui Song
Affiliation:1.Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China;2.The First Affiliated Hospital of Liaoning Medical University, Jinzhou 121001, China
Abstract:A series of novel 4-substituted-phenoxy-benzamide derivatives bearing an aryl cycloaliphatic amine moiety were synthesized and evaluated for antiproliferative activity against SW620, HT29 and MGC803 cancer cell lines in vitro. The pharmacological data demonstrated that the majority of target compounds exhibitedmoderate efficacy in HT29 and MGC803 cell lines. Compound 10c showed promising inhibition of hedgehog (Hh) signaling pathway in an Hh-related assay. In addition, the superposition pattern of 10c showed a good fit for a pharmacophoric model generated by Hh inhibitors and provided a basis for further structural optimization.
Keywords:Aryl cycloaliphatic amine  Antiproliferative activity  Hedgehog signaling  
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