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

被引：150

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 18期

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

页码：4711 / 4717

页数：7

共 26 条

[1]

AMBASTA SB, 1992, USEFUL PLANTS INDIA, P39

[2]

Anne M., 1991, J NATL CANCER I, V83, P757

[3] Inhibition of proprotein convertases-1, -7 and furin by diterpines of Andrographis paniculata and their succinoyl esters [J].