A variety of balanol analogs bearing carboxylic acid replacements (ami
des, sulfonamides and tetrazoles) were synthesized and evaluated for p
rotein kinase C (PKC) inhibitory activity. In general, those compounds
which bear an acidic proton (pKa less than or equal to 7.6) display p
otent PKC activity, and show selectivity for PKC over other kinases. P
rodrugs are excellent tools for increasing cellular activity of some a
cid replacements.