Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors
详细信息 查看全文
- 作者：Alex G. Waterson ; Kimberly G. Petrov ; Keith R. Hornberger ; Robert D. Hubbard ; Douglas M. Sammond ; Stephon C. Smith ; Hamilton D. Dickson ; Thomas R. Caferro ; Kevin W. Hinkle ; Kirk L. Stevens ; Scott H. D
- 关键词：Kinase inhibitor ; EGFR ; ErbB-2 ; Medicinal chemistry
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：1 March 2009
- 年：2009
- 卷：19
- 期：5
- 页码：1332-1336
- 全文大小：1350 K
文摘
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.