Bioorganic & medicinal chemistry letters

Novel matrix metallo-proteinase (MMP-2) phosphonoboronate inhibitors

I Pergament, R Reich, M Srebnik

Index: Pergament, Inna; Reich, Reuven; Srebnik, Morris Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 8 p. 1215 - 1218

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Citation Number: 16

Abstract

A series of novel phosphonoboronates consisting of PC 1 B, PC n B, PC(X)C n B, and PCC=CB derivatives were evaluated as MMP-2 inhibitors. Structure–activity relationships (SARs) data for the compounds were discovered and are discussed. ... The SAR of a group of novel phosphonoboronate MMP-2 inhibitors is reported. ... The use of both boronates and phosphonates as transition state analogue inhibitors is well known. 6 In addition, boronates were slow to ...