Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors

Autor:	Ta-Tung Yuan, Shyh-Fong Chen, Lee Tai Liu, Hung-Huang Liu, Ying-Ta Wu
Rok vydání:	2007
Předmět:	Models Molecular Stereochemistry Clinical Biochemistry Pharmaceutical Science Sonogashira coupling Antineoplastic Agents Biochemistry Chemical synthesis Inhibitory Concentration 50 Structure-Activity Relationship Gefitinib Drug Discovery medicine Structure–activity relationship Computer Simulation Molecular Biology IC50 EGFR inhibitors chemistry.chemical_classification Aniline Compounds Molecular Structure Organic Chemistry Aromatic amine In vitro ErbB Receptors chemistry Quinazolines Molecular Medicine Drug Screening Assays Antitumor medicine.drug
Zdroj:	Bioorganicmedicinal chemistry letters. 17(22)
ISSN:	0960-894X
Popis:	A series of C-6 or C-3′ alkynyl-substituted 4-anilinoquinazoline derivatives was prepared straightforwardly by a Sonogashira reaction of the corresponding bromo-substituted 4-anilinoquinazolines. Bioactive assay of these compounds for in vitro EGFR kinase inhibition demonstrated that the novel 6-hydroxypropynyl-4-anilinoquinazoline 5e was a very potent EGFR kinase inhibitor with an IC50 of 14 nM.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::92b245569ced442cb17bd9600535619c https://pubmed.ncbi.nlm.nih.gov/17889528 Zobrazit plný text záznamu Full Text from ScienceDirect