Novel PKC inhibitory analogs of balanol with replacement of the ester functionality

Balanol ((−)-1) is a potent protein kinase inhibitory natural product isolated from the fungus Verticillium balanoides. The presence of an ester functionality in this molecule has prompted concern over the metabolic stability of balanol, and has led to a search for active analogs lacking this moiety. The synthesis and serum stability for some of these is presented herein.

Balanol ((−)-) is a potent kinase inhibitory natural product isolated from the fungus Verticillium balanoides. The presence of an ester functionality in this molecule has prompted concern over the metabolic stability of balanol, and has led to a search for active analogs lacking this moiety. The synthesis and serum stability for some of these is presented herein.Figure optionsDownload as PowerPoint slide