Total synthesis and biological evaluation of nannocystin analogues modified at the polyketide phenyl moiety

被引:13
|
作者
Tian, Yunfeng
Ding, Yahui
Xu, Xiaolong
Bai, Yanju
Tang, Yang
Hao, Xin
Zhang, Weicheng [1 ]
Chen, Yue [1 ]
机构
[1] Nankai Univ, Coll Pharm, State Key Lab Med Chem Biol, Tianjin 300071, Peoples R China
基金
中国国家自然科学基金;
关键词
Nannocystin; Structure-activity relationship; Anticancer; Eukaryotic elongation factor 1A; CHONDRAMIDE-C; F-ACTIN; DIDEMNIN; AX;
D O I
10.1016/j.tetlet.2018.07.028
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Total synthesis of a focused set of 10 nannocystin analogues 3a-3j modified at the polyketide phenyl moiety was reported. These compounds were evaluated against three cancer cell lines. Compared with the naturally occurring congener 3a, the other synthetic variants either preserved or lose antiproliferative activity at varying degrees. Moreover, the potent analogues also displayed comparable levels of cytotoxicity toward two normal cell lines. (C) 2018 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3206 / 3209
页数:4
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