2,4-Disubstituted pyrimidines: A novel class of KDR kinase inhibitors

Autor:	George D. Hartman, Kenneth A. Thomas, Mark T. Bilodeau, Kathleen E. Coll, Keith W. Rickert, Leonard D. Rodman, Adrienne E. Balitza, Rosemary C. McFall, Peter J. Manley
Rok vydání:	2003
Předmět:	Stereochemistry Cell Clinical Biochemistry Pharmaceutical Science Angiogenesis Inhibitors Antineoplastic Agents Biochemistry Chemical synthesis Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Growth factor receptor parasitic diseases Drug Discovery medicine Humans Structure–activity relationship Enzyme Inhibitors neoplasms Molecular Biology Cells Cultured chemistry.chemical_classification biology Kinase Organic Chemistry General Medicine Vascular Endothelial Growth Factor Receptor-2 Pyrimidines medicine.anatomical_structure Enzyme chemistry Enzyme inhibitor cardiovascular system biology.protein Molecular Medicine Signal transduction Lead compound Derivative (chemistry) circulatory and respiratory physiology
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 13:1673-1677
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(03)00244-0
Popis:	2,4-Disubstituted pyrimidines were synthesized as a novel class of KDR kinase inhibitors. Evaluation of the SAR of the screening lead compound 1 (KDR IC(50)=105 nM, Cell IC(50)=8% inhibition at 500 nM) led to the potent 3,5-dimethylaniline derivative 2d (KDR IC(50)=6 nM, cell IC(50)=19 nM).
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::021d1bb9daf7639be702b1e7ab112c01 https://doi.org/10.1016/s0960-894x(03)00244-0 Zobrazit plný text záznamu Full Text from ScienceDirect