Title of article
Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases
Author/Authors
Harold Mastalerz، نويسنده , , Ming Chang، نويسنده , , Ashvinikumar Gavai، نويسنده , , Walter Johnson، نويسنده , , David Langley، نويسنده , , Francis Y. Lee، نويسنده , , Punit Marathe، نويسنده , , Arvind Mathur، نويسنده , , Simone Oppenheimer، نويسنده , , James Tarrant، نويسنده , , John S. Tokarski، نويسنده , , Gregory D. Vite، نويسنده , , Dolatrai M. Vyas، نويسنده , , Henry Wong، نويسنده , , Tai W. Wong، نويسنده , , Hongjian Zhang، نويسنده , , Guifen Zhang، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
6
From page
2828
To page
2833
Abstract
Novel C-5 aminomethyl pyrrolotriazines were prepared and optimized for dual EGFR and HER2 protein tyrosine kinase inhibition. The homopiperazine, 1p, emerged as a key lead and it showed promising oral efficacy in EGFR and dual EGFR/HER2 driven human tumor xenograft models. It is hypothesized that the C-5 homopiperazine side chain binds in the ribose–phosphate portion of the ATP binding pocket.
Keywords
Pyrrolotriazine , EGFR , HER2 , kinase inhibitor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798132
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