The synthesis of novel bisphosphonates as inhibitors of phosphoglycerate kinase (3-PGK)

…, CI Pogson, DJ Hayes, GM Blackburn

Index: Caplan, Neil A.; Pogson, Christopher I.; Hayes, David J.; Blackburn, G. Michael Journal of the Chemical Society, Perkin Transactions 1, 2000 , # 3 p. 421 - 437

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Citation Number: 11

Abstract

A series of conformationally-restrained analogues of 1, 3-bisphospho-D-glyceric acid (1, 3- BPG) 1 has been synthesised for use as inhibitors of 3-PGK (EC 2.7. 2.3). These compounds have non-scissile phosphonate linkages and also incorporate α-halogen substituents to make them isopolar and isosteric mimics of the natural substrate. A monocyclic aryl core between the two phosphoryl centres provides both a rigid framework linking these ...