Structural studies of cytotoxic marine alkaloids: Synthesis of novel ring-E analogues of ascididemin and their in vitro and in vivo biological evaluation

被引:25
作者
Lindsay, BS [1 ]
Christiansen, HC [1 ]
Copp, BR [1 ]
机构
[1] Univ Auckland, Dept Chem, Auckland, New Zealand
关键词
marine metabolites; structure-activity; antitumour compounds; alkaloids;
D O I
10.1016/S0040-4020(99)01038-8
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The cytotoxic marine alkaloid ascididemin and various pyridine ring-E analogues have been synthesised in an attempt to determine the pharmaceutical utility and structure-activity requirements for the parent alkaloid. All compounds synthesised were evaluated in a wide range of biological screens for selective cytotoxicity, antiviral, antifungal and antimicrobial properties. Many analogues exhibited selective cytotoxicity to human solid tumour cell-lines in vitro, with one also exhibiting moderate antitumour activity in in vivo xenograft assays. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:497 / 505
页数:9
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