Synthesis and structure-activity relationships of andrographolide analogues as novel cytotoxic agents

被引:145
|
作者
Nanduri, S
Nyavanandi, VK
Thunuguntla, SSR
Kasu, S
Pallerla, MK
Ram, PS
Rajagopal, S
Kumar, RA
Ramanujam, R
Babu, JM
Vyas, K
Devi, AS
Reddy, GO
Akella, V
机构
[1] Dr Reddys Labs Ltd, Discovery Res, Discovery Chem, Hyderabad 500049, Andhra Pradesh, India
[2] Dr Reddys Labs Ltd, Discovery Res, Discovery Biol, Hyderabad 500049, Andhra Pradesh, India
[3] Dr Reddys Labs Ltd, Discovery Res, Analyt Res, Hyderabad 500049, Andhra Pradesh, India
关键词
Andrographolide; Andrographis paniculata; cytotoxic agents;
D O I
10.1016/j.bmcl.2004.06.090
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Andrographolide 1, the cytotoxic agent of the plant Androgrophis paniculata was subjected to semi-synthetic studies leading to the preparation of a number of potent and novel analogues. Of the analogues synthesized, while 8,17-epoxy andrographolide 6 retained the cytotoxic activity of 1, ester derivatives of 6 exhibited considerable improvement in activity. Lower activity was observed when the epoxy moiety in the triacetate 9, derived from 6 was modified. Synthesis and structure-activity relationships are discussed. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4711 / 4717
页数:7
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