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