Ontology highlight
ABSTRACT:
SUBMITTER: McDermott LA
PROVIDER: S-EPMC6300166 | biostudies-literature | 2016 Apr
REPOSITORIES: biostudies-literature
McDermott Lee A LA Iyer Prema P Vernetti Larry L Rimer Shawn S Sun Jingran J Boby Melissa M Yang Tianyi T Fioravanti Michael M O'Neill Jason J Wang Liwei L Drakes Dylan D Katt William W Huang Qingqiu Q Cerione Richard R
Bioorganic & medicinal chemistry 20160307 8
A novel set of GAC (kidney glutaminase isoform C) inhibitors able to inhibit the enzymatic activity of GAC and the growth of the triple negative MDA-MB-231 breast cancer cells with low nanomolar potency is described. Compounds in this series have a reduced number of rotatable bonds, improved ClogPs, microsomal stability and ligand efficiency when compared to the leading GAC inhibitors BPTES and CB-839. Property improvements were achieved by the replacement of the flexible n-diethylthio or the n- ...[more]