Sigmond G. Johnson

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.

SELECTIVE INHIBITORS OF PROTEIN KINASE C IN A MODEL OF GRAFT-VS-HOST DISEASE

Abstract A series of 3-aryl-4-arylidene-5-isoxazolones were found to be active as inhibitors of PKC, and in ex-vivo and in vivo models of graft-versus-host disease.