title: Identification of novel pyrrolopyrazoles as protein kinase C β II inhibitors.
abstract: A novel series of pyrrolopyrazole-based protein kinase C β II inhibitors has been identified from high-throughput screening. Herein, we report our initial structure-activity relationship studies with a focus on optimizing compound ligand efficiency and physicochemical properties, which has led to potent inhibitors with good cell permeability.
authors.affiliation: Pfizer Global Research & Development, La Jolla Laboratories, 10770 Science Center Drive, San Diego, CA 92121, United States. hui.li@ppdi.com
authors.forename: Hui
authors.initials: H
authors.lastname: Li
authors.forename: Yufeng
authors.initials: Y
authors.lastname: Hong
authors.forename: Seiji
authors.initials: S
authors.lastname: Nukui
authors.forename: Jihong
authors.initials: J
authors.lastname: Lou
authors.forename: Sarah
authors.initials: S
authors.lastname: Johnson
authors.forename: Stephanie
authors.initials: S
authors.lastname: Scales
authors.forename: Iriny
authors.initials: I
authors.lastname: Botrous
authors.forename: Eileen
authors.initials: E
authors.lastname: Tompkins
authors.forename: Chunfeng
authors.initials: C
authors.lastname: Yin
authors.forename: Ru
authors.initials: R
authors.lastname: Zhou
authors.forename: Mingying
authors.initials: M
authors.lastname: He
authors.forename: Jordan
authors.initials: J
authors.lastname: Jensen
authors.forename: Djamal
authors.initials: D
authors.lastname: Bouzida
authors.forename: Gordon
authors.initials: G
authors.lastname: Alton
authors.forename: Jennifer
authors.initials: J
authors.lastname: Lafontaine
authors.forename: Stephan
authors.initials: S
authors.lastname: Grant
mesh_terms: D057166:High-Throughput Screening Assays; D011493:Protein Kinase C / Q000037:antagonists & inhibitors* / Q000378:metabolism; D064546:Protein Kinase C beta; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D011493:Protein Kinase C; D064546:Protein Kinase C beta