Studies on methyl xestopongoate analogues: design, synthesis and antitumor activities

被引：0
|
作者：
Sun Dongyu [1 ,2 ]
Gong Jingxu [2 ]
Li Xuwen [2 ]
Han Guanying [1 ,3 ]
Guo Yuewei [2 ]
机构：
[1] Jinzhou Med Univ, Sch Pharm, Jinzhou 121001, Peoples R China
[2] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
[3] Jinzhou Med Univ, Affiliated Hosp 1, Jinzhou 121001, Peoples R China
来源：
JOURNAL OF CHINA PHARMACEUTICAL UNIVERSITY | 2018年 / 49卷 / 04期
关键词：
Analogues; Antitumor activity; Methyl Xestospongoate; Polyacethlene; Synthesis;
D O I：
10.11665/j.issn.1000-5048.20180405
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Fifty-two methyl xestospongoate analogues were designed, synthesized and evaluated for the antiproliferative activity. Starting from alkynyl methyl ester and diyne, methyl xestospongoate analogues 4(a-m) - 7 (a-m) were synthesized by Cadiot-Chodkiewitz coupling and Sonogashira coupling reactions. Their structures were identified by H-1 NMR, C-13 NMR and HREI-MS. The cytotoxic inhibiton activities in vitro of some compounds were evaluated against human cancer cells A549 and P-388 by a CCK-8 method. Among them, compound 6k exhibited potent cell growth inhibitory activity against A549 and P-388 cancer cells, with IC50 values of 9. 36 and 9. 62 mu mol/L, respectively.
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收藏
页码：413 / 421
页数：9
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