Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1

…, S Sohal, J Golec, R Faint, T Brooks, P Charlton

Index: Folkes, Adrian; Roe, Michael B.; Sohal, Sukhjit; Golec, Julian; Faint, Richard; Brooks, Teresa; Charlton, Peter Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 19 p. 2589 - 2592

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Citation Number: 67

Abstract

We have synthesized and evaluated a series of diketopiperazine-based inhibitors of PAI-1. These studies resulted in the identification of 34 which inhibited PAI-1 in vitro with an IC 50 =0.2 μM. The synthesis and SAR of these compounds are described. ... We have synthesized and evaluated a series of diketopiperazine-based inhibitors of PAI-1. These studies resulted in the identification of 34 which inhibited PAI-1 in vitro with an IC 50 =0.2 μM. The synthesis and ...