e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
Design of alternate substrate inhibitors of serine proteases. Synergistic use of alkyl substitution to impede enzyme-catalyzed deacylation
…, RW Spencer, TF Tam, E Thomas…
Index: Krantz, Allen; Spencer, Robin W.; Tam, Tim F.; Thomas, Everton; Copp, Leslie J. Journal of Medicinal Chemistry, 1987 , vol. 30, # 4 p. 590 - 591
There is considerable interest in the design of stable small molecule inhibitors of serine proteases and in devising tactics to enhance the specificity and potency of such reagents. A particular challenge is to design specific inhibitors of high potency without resorting to peptide functionality as a means of delivering covalent labels to the target enzyme active site. 2 4H-3, 1-Benzoxazin-4-one (1) represents an attractive lead structure for ...
