Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors |
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Authors: | 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 Angel R Fuentes-Pesquera Steven A Middleton |
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Institution: | Johnson & Johnson Pharmaceutical Research & Development L.L.C., 1000 Route 202, Raritan, NJ 08869, USA |
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Abstract: | 2,7-Diamino-thiazolo4,5-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. |
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