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Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a
Diane E Gingrich1, Robert L Hudkins
1Department of Medicinal Chemistry, Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA 19380, USA. dgingric@cephalon.com
Bioorganic & Medicinal Chemistry Letters
|September 25, 2002
Abstract:
The 3'-epi diastereomer of K-252a was synthesized with the goal of evaluating the stereochemical requirements of the 3'-sugar alcohol on kinase inhibitory activity. Inverting the 3'-alcohol resulted in a 20 nM inhibitor of VEGFR2 and a 1 nM inhibitor of TrkA tyrosine kinase.