Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1 |
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Authors: | Folkes A Roe M B Sohal S Golec J Faint R Brooks T Charlton P |
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Affiliation: | Xenova Limited, 957 Buckingham Avenue, Slough, Berks SL1 4NL, UK. adrian_folkes@xenova.co.uk |
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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 microM. The synthesis and SAR of these compounds are described. |
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