Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors

Autor:	Kimberly G. Petrov, Thomas R. Caferro, Octerloney B. McDonald, David W. Rusnak, Dana E. Vanderwall, Kelly Horne Donaldson, Tara Renae Rheault, David E. Uehling, Lisa M. Shewchuk, Scott Howard Dickerson, Robert J. Mullin, Michael D. Gaul, Aaron S. Goetz, Glenn M. Spehar, Anne T. Truesdale, Edgar R. Wood
Rok vydání:	2009
Předmět:	Pyrimidine Receptor ErbB-2 Stereochemistry Chemistry Pharmaceutical Clinical Biochemistry Molecular Conformation Pharmaceutical Science Antineoplastic Agents Lapatinib Biochemistry Sulfone Inhibitory Concentration 50 chemistry.chemical_compound ErbB Cell Line Tumor Drug Discovery medicine Humans Epidermal growth factor receptor Enzyme Inhibitors Molecular Biology Cell Proliferation biology Chemistry Kinase Organic Chemistry In vitro ErbB Receptors Pyrimidines Models Chemical Enzyme inhibitor Drug Design Quinazolines biology.protein Molecular Medicine Drug Screening Assays Antitumor medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 19:817-820
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2008.12.011
Popis:	Two new series of potent and selective dual EGFR/ErbB-2 kinase inhibitors derived from novel thienopyrimidine cores have been identified. Isomeric thienopyrimidine cores were evaluated as isosteres for a 4-anilinoquinazoline core and several analogs containing the thieno[3,2-d]pyrimidine core showed anti-proliferative activity with IC(50) values less than 1 microM against human tumor cells in vitro.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8a62e1d36d5f76869f6a2a75d7237e2 https://doi.org/10.1016/j.bmcl.2008.12.011 Zobrazit plný text záznamu Full Text from ScienceDirect