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

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: 29 May 2015
Fund Project:

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.
- Aryl cycloaliphatic amine,
- Antiproliferative activity,
- Hedgehog signaling
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沈阳化工大学材料科学与工程学院沈阳 110142