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. 2008 Apr 15;18(8):2691-5.
doi: 10.1016/j.bmcl.2008.03.021. Epub 2008 Mar 10.

Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors

Vijaya Gracias  1 , Zhiqin Ji, Irini Akritopoulou-Zanze, Cele Abad-Zapatero, Jeffrey R Huth, Danying Song, Philip J Hajduk, Eric F Johnson, Keith B Glaser, Patrick A Marcotte, Lori Pease, Nirupama B Soni, Kent D Stewart, Steven K Davidsen, Michael R Michaelides, Stevan W Djuric
Affiliations

Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors

Vijaya Gracias et al. Bioorg Med Chem Lett. .

Abstract

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 (IC(50)=9 and 52 nM, respectively).

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