Synthesis and antiproliferative activity of novel 4-substituted-phenoxy-benzamide derivatives |
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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 |
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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 |
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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. |
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Keywords: | Aryl cycloaliphatic amine Antiproliferative activity Hedgehog signaling |
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