Literature DB >> 17270437

New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Harold Mastalerz1, Ming Chang, Ping Chen, Pierre Dextraze, Brian E Fink, Ashvinikumar Gavai, Bindu Goyal, Wen-Ching Han, Walter Johnson, David Langley, Francis Y Lee, Punit Marathe, Arvind Mathur, Simone Oppenheimer, Edward Ruediger, James Tarrant, John S Tokarski, Gregory D Vite, Dolatrai M Vyas, Henry Wong, Tai W Wong, Hongjian Zhang, Guifen Zhang.   

Abstract

Novel C-5 substituted pyrrolotriazines were optimized for dual EGFR and HER2 protein tyrosine kinase inhibition. The lead compound exhibited promising oral efficacy in both EGFR and HER2 driven human tumor xenograft models. It is hypothesized that its C-5 morpholine side chain binds in the ribose phosphate portion of the ATP binding pocket.

Entities:  

Mesh:

Substances:

Year:  2007        PMID: 17270437     DOI: 10.1016/j.bmcl.2007.01.002

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Identifying HER2 inhibitors from natural products database.

Authors:  Shun-Chieh Yang; Su-Sen Chang; Calvin Yu-Chian Chen
Journal:  PLoS One       Date:  2011-12-12       Impact factor: 3.240

2.  Organic-inorganic nanocrystal reductase to promote green asymmetric synthesis.

Authors:  Kotchakorn T Sriwong; Afifa Ayu Koesoema; Tomoko Matsuda
Journal:  RSC Adv       Date:  2020-08-20       Impact factor: 4.036

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.