title: Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1.
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.
authors.affiliation: Xenova Limited, 957 Buckingham Avenue, Slough, Berks SL1 4NL, UK. adrian_folkes@xenova.co.uk
authors.forename: A
authors.initials: A
authors.lastname: Folkes
authors.forename: M B
authors.initials: MB
authors.lastname: Roe
authors.forename: S
authors.initials: S
authors.lastname: Sohal
authors.forename: J
authors.initials: J
authors.lastname: Golec
authors.forename: R
authors.initials: R
authors.lastname: Faint
authors.forename: T
authors.initials: T
authors.lastname: Brooks
authors.forename: P
authors.initials: P
authors.lastname: Charlton
mesh_terms: D054659:Diketopiperazines; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017395:Plasminogen Activator Inhibitor 1 / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D054659:Diketopiperazines; D010879:Piperazines; D017395:Plasminogen Activator Inhibitor 1; C107761:XR 5118