Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors

  • Bioorg Med Chem Lett. 2009 Feb 1;19(3):817-20. doi: 10.1016/j.bmcl.2008.12.011.
Tara R Rheault  1 ,  Thomas R Caferro ,  Scott H Dickerson ,  Kelly H Donaldson ,  Michael D Gaul ,  Aaron S Goetz ,  Robert J Mullin ,  Octerloney B McDonald ,  Kimberly G Petrov ,  David W Rusnak ,  Lisa M Shewchuk ,  Glenn M Spehar ,  Anne T Truesdale ,  Dana E Vanderwall ,  Edgar R Wood ,  David E Uehling
Affiliations
  • 1. Department of Oncology Medicinal Chemistry, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA. [email protected]
PMID: 19111461 DOI: 10.1016/j.bmcl.2008.12.011
Abstract

Two new series of potent and selective dual EGFR/ErbB-2 kinase inhibitors derived from novel thienopyrimidine cores have been identified. Isomeric thienopyrimidine cores were evaluated as isosteres for a 4-anilinoquinazoline core and several analogs containing the thieno[3,2-d]pyrimidine core showed anti-proliferative activity with IC(50) values less than 1 microM against human tumor cells in vitro.

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