1029135-27-0Relevant articles and documents
Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors
Gracias, Vijaya,Ji, Zhiqin,Akritopoulou-Zanze, Irini,Abad-Zapatero, Cele,Huth, Jeffrey R.,Song, Danying,Hajduk, Philip J.,Johnson, Eric F.,Glaser, Keith B.,Marcotte, Patrick A.,Pease, Lori,Soni, Nirupama B.,Stewart, Kent D.,Davidsen, Steven K.,Michaelides, Michael R.,Djuric, Stevan W.
, p. 2691 - 2695 (2008/12/21)
We report the discovery of the pyrimido-diazepine scaffolds as novel adenine mimics. Structure-based design led to the discovery of analogs with potent inhibitory activity against receptor tyrosine kinases, such as KDR, Flt3 and c-Kit. Compound 14 exhibited low nanomolar KDR enzymatic and cellular potencies (IC50 = 9 and 52 nM, respectively).
