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ID: ALA1131405

Journal: Bioorg Med Chem Lett

Title: Novel bisphosphonate inhibitors of phosphoglycerate kinase.

Authors: Caplan NA, Pogson CI, Hayes DJ, Blackburn GM.

Abstract: A series of novel, conformationally-restrained bisphosphonate analogues of 1,3-bisphosphoglyceric acid 1 have been synthesised and evaluated as inhibitors of 3-PGK. They are competitive inhibitors of the human enzyme and, especially for certain alpha-halophosphonic acid analogues, both Ki and IC50 values extend into the submicromolar range.

CiteXplore: 9871609

DOI: 10.1016/s0960-894x(98)00059-6