Preparation and optimization of new 4-(2-(indolin-1-yl)-2-oxoethyl)-2-morpholinothiazole-5-carboxylic acid and amide derivatives as potent and selective PI3Kβ inhibitors

Autor:	Christoph Lengauer, Pierre Yves Abecassis, Luc Bertin, Véronique Charrier, Laurent Schio, Jean Christophe Carry, Patrick Richepin, Loic Vincent, Bruno Filoche-Romme, Florence Gruss-Leleu, Houlfa Guizani, Carlos Garcia-Echeverria, Angela Virone-Oddos, Andreas Karlsson, Jean Paul Nicolas, Victor Certal, Fabienne Pilorge, Frank Halley
Rok vydání:	2014
Předmět:	Male Indoles Stereochemistry Carboxylic acid Clinical Biochemistry Carboxylic Acids Pharmaceutical Science Biochemistry Permeability Rats Sprague-Dawley chemistry.chemical_compound Phosphatidylinositol 3-Kinases Amide Drug Discovery Animals Humans Protein Isoforms Thiazole Molecular Biology Protein Kinase Inhibitors Phosphoinositide-3 Kinase Inhibitors chemistry.chemical_classification Binding Sites Organic Chemistry Combinatorial chemistry Amides Protein Structure Tertiary Rats Molecular Docking Simulation Thiazoles chemistry Molecular Medicine Caco-2 Cells Proto-Oncogene Proteins c-akt
Zdroj:	Bioorganicmedicinal chemistry letters. 24(6)
ISSN:	1464-3405
Popis:	In our continuous efforts to identify and develop novel targeted cancer treatments, a new morpholino-thiazole scaffold active against PI3Kβ has been identified. This Letter reports the optimization of this compound class to develop PI3Kβ isoform-selective inhibitors with suitable pharmacological properties.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77a5914bd72703a797db886448147528 https://pubmed.ncbi.nlm.nih.gov/24560540 Zobrazit plný text záznamu Full Text from ScienceDirect