7-Phenyl-pyrido[2,3-d]pyrimidine-2,4-diamines: Novel and highly selective protein tyrosine phosphatase 1B inhibitors

Autor:	Kshitij Chhabilbhai Thakkar, Bruce L. Banner, Shiming Li, Nicholas Marcopulos, Joseph A. Sergi, Jolly Bose, Weiya Yun, Catherine Zwingelstein, Adrian Wai-Hing Cheung, Kyungjin Kim, Steven Joseph Berthel, Bingbing Wang, Lucja Orzechowski, Andrée R. Olivier
Rok vydání:	2012
Předmět:	Pyrimidine Stereochemistry High-throughput screening Clinical Biochemistry Phosphatase Pharmaceutical Science Protein tyrosine phosphatase Diamines Biochemistry Mice Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Animals Humans Enzyme Inhibitors Molecular Biology Protein Tyrosine Phosphatase Non-Receptor Type 1 Dose-Response Relationship Drug Molecular Structure Chemistry Organic Chemistry Highly selective Protein Tyrosine Phosphatase 1B Mice Inbred C57BL Pyrimidines Molecular Medicine hormones hormone substitutes and hormone antagonists
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 22:7518-7522
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2012.10.035
Popis:	High throughput screening of the Roche compound collection led to the identification of diaminopyrroloquinazoline series as a novel class of PTP1B inhibitors. Structural modification of diaminopyrroloquinazoline series resulted in pyrido[2,3-d]pyrimidine-2,4-diamine series which was further optimized to give compounds 5 and 24 as potent, selective (except T-cell phosphatase) PTP1B inhibitors with good mouse PK properties.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c232213a45381b928aa7b22c684842bc https://doi.org/10.1016/j.bmcl.2012.10.035 Zobrazit plný text záznamu Full Text from ScienceDirect