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Bioorg Med Chem Lett. 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.

Author information

1
Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60044, USA.

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).

PMID:
18362070
DOI:
10.1016/j.bmcl.2008.03.021
[Indexed for MEDLINE]

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