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4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.

Abstract：

:Inhibitors of human methionine aminopeptidase type 2 (hMetAP2) are of interest as potential treatments for cancer. A new class of small molecule reversible inhibitors of hMetAP2 was discovered and optimized, the 4-aryl-1,2,3-triazoles. Compound 24, a potent inhibitor of cobalt-activated hMetAP2, also inhibits human and mouse endothelial cell growth. Using a mouse matrigel model, this reversible hMetAP2 inhibitor was also shown to inhibit angiogenesis in vivo.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Kallander LS,Lu Q,Chen W,Tomaszek T,Yang G,Tew D,Meek TD,Hofmann GA,Schulz-Pritchard CK,Smith WW,Janson CA,Ryan MD,Zhang GF,Johanson KO,Kirkpatrick RB,Ho TF,Fisher PW,Mattern MR,Johnson RK,Hansbury MJ,Winkler JD,

doi

10.1021/jm050408c

keywords:

subject

Has Abstract

pub_date

2005-09-08 00:00:00

pages

5644-7

issue

18

eissn

0022-2623

issn

1520-4804

journal_volume

48

pub_type

杂志文章

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