Scabrosin esters and derivatives: chemical derivatization studies and biological evaluation

被引:17
作者
Chai, CLL [1 ]
Elix, JA [1 ]
Huleatt, PB [1 ]
Waring, P [1 ]
机构
[1] Australian Natl Univ, Dept Chem, Ctr Study Bioact Mol, Canberra, ACT 0200, Australia
基金
澳大利亚研究理事会;
关键词
anti-proliferative agents; anti-tumour compounds; natural products; polycyclic heterocyclic compounds;
D O I
10.1016/j.bmc.2004.08.015
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Several derivatives of the natural scabrosin esters were synthesized in order to elucidate the structural features present, which are responsible for the biological activities. The studies demonstrate that full anti-proliferative activities of the scabrosin esters, both the carboskeleton core as well as the ability to form the dithiol and/or the disulfide linkage of the epidithiopiperazine-2,5-dione are required. The presence of the epoxide rings on the scabrosin esters do not contribute to the observed biological activities. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5991 / 5995
页数:5
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