Acylated Gly-(2-cyano) pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity

…, I De Meester, K Augustyns, P Van der Veken

文献索引：Ryabtsova, Oxana; Jansen, Koen; Van Goethem, Sebastiaan; Joossens, Jurgen; Cheng, Jonathan D.; Lambeir, Anne-Marie; De Meester, Ingrid; Augustyns, Koen; Van Der Veken, Pieter Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 10 p. 3412 - 3417

全文：HTML全文

被引用次数: 7

摘要

A series of N-acylated glycyl-(2-cyano) pyrrolidines were synthesized with the aim of generating structure–activity relationship (SAR) data for this class of compounds as inhibitors of fibroblast activation protein (FAP). Specifically, the influence of (1) the choice of the N-acyl group and (2) structural modification of the 2-cyanopyrrolidine residue were investigated. The inhibitors displayed inhibitory potency in the micromolar to nanomolar ...