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

被引:5
作者
Sun, Chi-Yu [1 ]
Li, Yang-Sheng [1 ]
Shi, Ai-Long [1 ]
Li, Ya-Fei [1 ]
Cao, Rui-Fang [1 ]
Ding, Huai-Wei [1 ]
Yin, Qing-Qing [1 ]
Zhang, Li-Juan [1 ]
Zheng, Hua-Chuan [2 ]
Song, Hong-Rui [1 ]
机构
[1] Shenyang Pharmaceut Univ, Minist Educ, Key Lab Struct Based Drug Design & Discovery, Shenyang 110016, Peoples R China
[2] Liaoning Med Univ, Affiliated Hosp 1, Jinzhou 121001, Peoples R China
关键词
Aryl cycloaliphatic amine; Antiproliferative activity; Hedgehog signaling; HEDGEHOG SIGNALING PATHWAY; BASAL-CELL CARCINOMA; INHIBITORS; DISCOVERY; DESIGN; ANTAGONISTS; IDENTIFICATION; VISMODEGIB; CANCER; POTENT;
D O I
10.1016/j.cclet.2015.06.017
中图分类号
O6 [化学];
学科分类号
0703 ;
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 exhibited moderate 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. (C) 2015 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.
引用
收藏
页码:1307 / 1310
页数:4
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