Studies on methyl xestopongoate analogues:design, synthesis and antitumor activities
10.11665/j.issn.1000-5048.20180405
- VernacularTitle:Methyl Xestospongoate类似物的设计、合成和抗肿瘤活性
- Author:
Dongyu SUN
1
;
Jingxu GONG
;
Xuwen LI
;
Guanying HAN
;
Yuewei GUO
Author Information
1. 锦州医科大学药学院；中国科学院上海药物研究所新药研究国家重点实验室
- Publication Type:Journal Article
- Keywords:
Methyl Xestospongoate;
polyacethlene;
analogues;
synthesis;
antitumor activity
- From:
Journal of China Pharmaceutical University
2018;49(4):413-421
- CountryChina
- Language:Chinese
-
Abstract:
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 1H NMR, 13C 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 μmol/L, respectively.
