Inhibition of PI3Kd is considered to be an attractive mechanism for the treatment of inflammatory diseases and leukocyte malignancies.  Using a structure-based design approach, we have identified a series of potent and selective benzimidazole-based inhibitors of PI3Kd.  These inhibitors do not occupy the selectivity pocket between Trp760 and Met752 that is induced by other families of PI3Kd inhibitors.  The pharmacokinetic properties of these compounds and the ability of representative inhibitors to modulate the function of B-cells in vivo will be described.

Potent and highly selective benzimidazole inhibitors of PI3-Kinase delta

242nd National Meeting (2011)

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