Document Report Card

ID: ALA1145806

Journal: J Med Chem

Title: Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae.

Authors: Luo QL, Li JY, Liu ZY, Chen LL, Li J, Qian Z, Shen Q, Li Y, Lushington GH, Ye QZ, Nan FJ.

Abstract: A series of pyridine-2-carboxylic acid derivatives were synthesized according to the leads from the screening, and potent inhibitors have been obtained by structural modification. They have shown submicromolar inhibition of the enzymes (for example, for 9n, IC(50) = 130 nM for EcMetAP1 and IC(50) = 380 nM for ScMetAP1). They represent small-molecule MetAP inhibitors with novel structures different from alkylating fumagillin derivatives and peptidic bestatin-based MetAP inhibitor.

CiteXplore: 12801227

DOI: 10.1021/jm0300532