title: Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors.
abstract: 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.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development LLC, Raritan, NJ 08869, USA. Ronghui.Lin@yahoo.com
authors.forename: Ronghui
authors.initials: R
authors.lastname: Lin
authors.forename: Sigmond G
authors.initials: SG
authors.lastname: Johnson
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Connolly
authors.forename: Steven K
authors.initials: SK
authors.lastname: Wetter
authors.forename: Eva
authors.initials: E
authors.lastname: Binnun
authors.forename: Terry V
authors.initials: TV
authors.lastname: Hughes
authors.forename: William V
authors.initials: WV
authors.lastname: Murray
authors.forename: Niranjan B
authors.initials: NB
authors.lastname: Pandey
authors.forename: Sandra J
authors.initials: SJ
authors.lastname: Moreno-Mazza
authors.forename: Mary
authors.initials: M
authors.lastname: Adams
authors.forename: Angel R
authors.initials: AR
authors.lastname: Fuentes-Pesquera
authors.forename: Steven A
authors.initials: SA
authors.lastname: Middleton
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D066246:ErbB Receptors