5-Substituted 4-anilinoquinazolines as potent, selective and orally active inhibitors of erbB2 receptor tyrosine kinase

Autor:	Rémy Morgentin, Peter Ballard, D. Mark Hickinson, Laurent Francois Andre Hennequin, Johnson Paul David, Donald J. Ogilvie, Robert Hugh Bradbury, Teresa Klinowska, Jason Grant Kettle, Annie Olivier
Rok vydání:	2005
Předmět:	Transplantation Heterologous Clinical Biochemistry Administration Oral Pharmaceutical Science Antineoplastic Agents Biochemistry Receptor tyrosine kinase Inhibitory Concentration 50 Mice Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Quinazoline Animals Structure–activity relationship Epidermal growth factor receptor Enzyme Inhibitors Molecular Biology chemistry.chemical_classification biology Organic Chemistry Intracellular Signaling Peptides and Proteins Neoplasms Experimental Tumor Burden Transplantation Enzyme chemistry Enzyme inhibitor Quinazolines biology.protein Molecular Medicine Signal transduction Carrier Proteins
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 15:4226-4229
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2005.06.068
Popis:	Starting from a 6,7-substituted quinazoline lead 4, optimisation of 5-substituted quinazolines containing an extended aniline motif led to potent and selective inhibitors of erbB2 receptor tyrosine kinase, and a representative compound 12a inhibited tumour growth in a mouse xenograft model.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::96829569526116303bbf291985fb43e9 https://doi.org/10.1016/j.bmcl.2005.06.068 Zobrazit plný text záznamu Full Text from ScienceDirect