2. Academic Validation
  3. Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays

Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays

  • Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. doi: 10.1016/j.bmcl.2006.11.006.
Glenn Noronha 1,  Kathy Barrett,  Antonio Boccia,  Tessa Brodhag,  Jianguo Cao,  Chun P Chow,  Elena Dneprovskaia,  John Doukas,  Richard Fine,  Xianchang Gong,  Colleen Gritzen,  Hong Gu,  Ehab Hanna,  John D Hood,  Steven Hu,  Xinshan Kang,  Jann Key,  Boris Klebansky,  Ahmed Kousba,  Ge Li,  Dan Lohse,  Chi Ching Mak,  Andrew McPherson,  Moorthy S S Palanki,  Ved P Pathak,  Joel Renick,  Feng Shi,  Richard Soll,  Ute Splittgerber,  Silva Stoughton,  Suhan Tang,  Shiyin Yee,  Binqi Zeng,  Ningning Zhao,  Hong Zhu
Affiliations

Affiliation

PMID: 17113292 DOI: 10.1016/j.bmcl.2006.11.006
Abstract

We describe the identification of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine (3), a potent, orally active Src Inhibitor with desirable PK properties, demonstrated activity in human tumor cell lines and in animal models of tumor growth.

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