Synthesis and antiproliferative activity of novel 4-substituted-phenoxy-benzamide derivatives

注册 English

Synthesis and antiproliferative activity of novel 4-substituted-phenoxy-benzamide derivatives

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

Citation: 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. Synthesis and antiproliferative activity of novel 4-substituted-phenoxy-benzamide derivatives[J]. Chinese Chemical Letters, 2015, 26(10): 1307-1310. doi: 10.1016/j.cclet.2015.06.017 shu

shu

Synthesis and antiproliferative activity of novel 4-substituted-phenoxy-benzamide derivatives

通讯作者: Huai-Wei Ding,
Hong-Rui Song,

基金项目:

entrepreneurship training program for college students in Liaoning Province (No. 201410163009). (No. 201410163009)

摘要: 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.

关键词:

English

Synthesis and antiproliferative activity of novel 4-substituted-phenoxy-benzamide derivatives

1.
1 Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China;
2.
2 The First Affiliated Hospital of Liaoning Medical University, Jinzhou 121001, China

Corresponding author: Huai-Wei Ding, Hong-Rui Song,

Received Date: 24 March 2015
Available Online: 20 June 2015

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.

Key words:

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