Description
Ketomethylenebestatin is a carba-analogue of the aminopeptidase (AP) inhibitor bestatin. This synthesis was carried out by a malonic ester alkylation with the suitably protected halomethyl ketone of (2S,3R)-AHPBA*), followed by a second alkylation with isobutyl bromide of the resulting 4-ketodiester, and subsequent decarboxylation and deprotection. Ketomethylenebestatin is 10 fold less effective as inhibitor of aminopeptidases than bestatin.
Uses
Ketomethylenebestatin is an aminopeptidase (AP) inhibitor and an analog of the natural aminopeptidase inhibitor Bestatin (HY-B0134) with IC50 of 56 μM, 752 μM and 0.39 μM for AP-B, AP-M and Leu-AP, respectively[1].
