Synthesis and evaluation of a novel series of indoloisoquinolines as small molecule anti-malarial leads

被引：17

作者：

Horrocks, Paul ^{[3
,4
]}

Fallon, Samantha ^{[1
,2
]}

Denman, Laura ^{[3
]}

Devine, Oliver ^{[3
]}

Duffy, Liam J. ^{[1
,2
,4
]}

Harper, Anthony ^{[5
]}

Meredith, Emma-Louise ^{[5
]}

Hasenkamp, Sandra ^{[4
]}

Sidaway, Adam ^{[5
]}

Monnery, Daniel ^{[3
]}

Phillips, Theresa R. ^{[1
,2
]}

Allin, Steven M. ^{[1
,2
]}

机构：

[1] Keele Univ, Sch Phys & Geog Sci, Keele ST5 5BG, Staffs, England

[2] Keele Univ, Inst Environm Phys Sci & Math, Keele ST5 5BG, Staffs, England

[3] Keele Univ, Sch Med, Keele ST5 5BG, Staffs, England

[4] Keele Univ, Inst Sci & Technol Med, Keele ST5 5BG, Staffs, England

[5] Keele Univ, Sch Life Sci, Keele ST5 5BG, Staffs, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 04期

基金：

英国工程与自然科学研究理事会; 英国惠康基金;

关键词：

Indoloisoquinoline; Anti-malarial; Natural product; Malaria; Dihydrousambarensine; PLASMODIUM-FALCIPARUM; ASYMMETRIC-SYNTHESIS; ALKALOIDS; CULTURE; MALARIA; AGENTS;

D O I：

10.1016/j.bmcl.2011.12.071

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A group of novel synthetic indoloisoquinolines was prepared and its potential as a novel series of smallmolecule anti-malarial leads was assessed. The structure-activity relationship on variation of three distinct regions of chemical space was investigated. A lead compound was generated with an activity close to that observed for a known anti-malarial natural product, dihydrousambarensine, that shares the indoloisoquinoline template structure. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：1770 / 1773

页数：4

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