529509-36-2Relevant academic research and scientific papers
Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases
Mastalerz, Harold,Chang, Ming,Gavai, Ashvinikumar,Johnson, Walter,Langley, David,Lee, Francis Y.,Marathe, Punit,Mathur, Arvind,Oppenheimer, Simone,Tarrant, James,Tokarski, John S.,Vite, Gregory D.,Vyas, Dolatrai M.,Wong, Henry,Wong, Tai W.,Zhang, Hongjian,Zhang, Guifen
, p. 2828 - 2833 (2007)
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.
C-5 Modified indazolylpyrrolotriazines
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, (2008/06/13)
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
