Synthesis and kinase inhibitory activity of 3′-(S)-epi-K-252a

Bioorganic & Medicinal Chemistry Letters
2002.0

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.

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