Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: Design, synthesis and biological activity

Autor:	Richard I. Feldman, Gary Phillips, Marc Adler, Daguang Zhu, Elena Ho, Wheeseong Lee, Mark A. Polokoff, Hongyi Yu, Dao Lentz, Marc Whitlow, Arnaiz Damian O, Kochanny Monica, Babu Subramanyam, Imadul Islam, James M. Wu, Judi Bryant, Yuo-Ling Chou
Rok vydání:	2007
Předmět:	Models Molecular Indoles animal structures Clinical Biochemistry Pharmaceutical Science Protein Serine-Threonine Kinases Biochemistry Chemical synthesis 3-Phosphoinositide-Dependent Protein Kinases Drug Discovery Transferase Protein kinase A Protein Kinase Inhibitors Molecular Biology Protein kinase B Molecular Structure biology Chemistry Organic Chemistry Biological activity Enzyme inhibitor Drug Design biology.protein Molecular Medicine Signal transduction Phosphoinositide-dependent kinase-1
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 17:3814-3818
ISSN:	0960-894X
Popis:	HTS screening identified 1 with micromolar inhibitory activity against PDK1. Optimization of 1 afforded 4i (BX-517) which has single-digit nanomolar activity against PDK1 and excellent selectivity against PKA.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca9b5b6c85e996a38c96e34d7d0210bc https://doi.org/10.1016/j.bmcl.2007.04.071 Zobrazit plný text záznamu Full Text from ScienceDirect