Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase 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.
Lin
Ronghui
R
Johnson & Johnson Pharmaceutical Research & Development LLC, Raritan, NJ 08869, USA. Ronghui.Lin@yahoo.com
Johnson
Sigmond G
SG
Connolly
Peter J
PJ
Wetter
Steven K
SK
Binnun
Eva
E
Hughes
Terry V
TV
Murray
William V
WV
Pandey
Niranjan B
NB
Moreno-Mazza
Sandra J
SJ
Adams
Mary
M
Fuentes-Pesquera
Angel R
AR
Middleton
Steven A
SA
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
D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D066246:ErbB Receptors