Potent blockers of the monocarboxylate transporter MCT1: Novel immunomodulatory compounds

被引：43

作者：

Guile, SD

Banticka, JR

Cheshire, DR

Cooper, ME

Davis, AM

Donald, DK

Evans, R

Eyssade, C

Ferguson, DD

Hill, S

Hutchinson, R

Ingall, AH

Kingston, LP

Martin, I

Martin, BP

Mohammed, RT

Murray, C

Perry, MWD

Reynolds, RH

Thorne, PV

Wilkinson, DJ

Withnall, J

机构：

[1] AstraZeneca R&D Charnwood, Dept Med Chem, Loughborough LE11 5RH, Leics, England

[2] AstraZeneca R&D Charnwood, Dept Phys & Metab Sci, Loughborough LE11 5RH, Leics, England

[3] AstraZeneca R&D Charnwood, Dept Discovery Biosci, Loughborough LE11 5RH, Leics, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 08期

关键词：

monocarboxylate; transporter; immunomodulatory;

D O I：

10.1016/j.bmcl.2006.01.024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of potent blockers of the monocarboxylate transporter, MCT1, is disclosed. From very potent but lipophilic lead compounds, systematic changes to all parts of the molecule, targeting reduction in log D, afforded compounds with significantly improved overall properties. These Compounds show potent immunomodulatory activity. (C) 2006 Elsevier Ltd. All rights reserved.

引用

收藏

页码：2260 / 2265

页数：6

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