Sign in
Back
Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
Journal article   Peer reviewed

Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors

Ronghui Lin, Sigmond G Johnson, Peter J Connolly, Steven K Wetter, Eva Binnun, Terry V Hughes, William V Murray, Niranjan B Pandey, Sandra J Moreno-Mazza, Mary Adams, …
Bioorganic & medicinal chemistry letters, Vol.19(8), pp.2333-2337
15/04/2009
DOI: https://doi.org/10.1016/j.bmcl.2009.02.067
PMID: 19286381

Abstract

Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Cell Line, Tumor Cell Proliferation - drug effects Drug Screening Assays, Antitumor - methods Humans Protein Kinase Inhibitors - analogs & derivatives Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - pharmacology Pyrimidines - chemical synthesis Pyrimidines - pharmacology Receptor, Epidermal Growth Factor - antagonists & inhibitors
2,7-Diamino-thiazolo[4,5-d]pyrimidine analogues were synthesized as novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Representative compounds showed potent and selective EGFR inhibitory activities and inhibited in vitro cellular proliferation in EGFR-overexpressing human tumor cells. The synthesis and preliminary biological, physical, and pharmacokinetic evaluation of these thiazolopyrimidine compounds are reported.

Metrics

1 Record Views

Details