| Literature DB >> 18362070 |
Vijaya Gracias1, 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.
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).Entities:
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Year: 2008 PMID： 18362070 DOI： 10.1016/j.bmcl.2008.03.021
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823