2. Academic Validation
  3. Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors

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

Affiliation

  • 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.

Figures
Products