Document Report Card
Basic Information
ID: ALA1153281
Journal: Bioorg Med Chem Lett
Title: Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors.
Authors: Waterson AG, Petrov KG, Hornberger KR, Hubbard RD, Sammond DM, Smith SC, Dickson HD, Caferro TR, Hinkle KW, Stevens KL, Dickerson SH, Rusnak DW, Spehar GM, Wood ER, Griffin RJ, Uehling DE.
Abstract: Aniline 'headgroups' were synthesized and incorporated into an alkynyl thienopyrimidine series of EGFR and ErbB-2 inhibitors. Potent inhibition of enzyme activity and cellular proliferation was observed. In certain instances, protein binding was reduced and oral exposure was found to be somewhat improved relative to compounds containing the reference aniline.
CiteXplore: 19208477