Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits

…, JS Mendoza, MM Murphy, JW Wilson…

Index: Lampe, John W.; Jagdmann Jr., G. Erik; Johnson, Mary George; Lai, Yen-Shi; Lowden, Christopher T.; Lynch, Michael P.; Mendoza, Jose S.; Murphy, Marcia M.; Wilson, Joseph W.; Ballas, Lawrence M.; Carter, Kiyomi; Biggers, Christopher K.; Darges, James W.; Davis, Jefferson E.; Hubbard, Frederick R.; Stamper, Mark L.; Defauw, Jean M.; Foglesong, Robert J.; Hall, Steven E.; Heerding, Julia M.; Hollinshead, Sean P.; Hu, Hong; Hughes, Philip F. Journal of Medicinal Chemistry, 2002 , vol. 45, # 12 p. 2624 - 2643

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Citation Number: 46

Abstract

A series of analogues of the protein kinase C (PKC) inhibitory natural product balanol which bear modified benzophenone subunits are described. The analogues were designed with the goal of uncovering structure-activity features that could be used in the development of PKC inhibitors with a reduced polar character compared to balanol itself. The results of these studies suggest that most of the benzophenone features found in the natural product ...