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
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.