Protein kinase C modulators bearing dicarba-closo-dodecaborane as a hydrophobic pharmacophore

The size and position of a hydrophobic moiety on a benzolactam skeleton, wh ich reproduces the active conformation and biological activity of teleocidi ns, play an important role in the appearance of the activity. We have desig ned and synthesized benzolactams bearing dicarba-closo-dodecaborane. These compounds showed potent binding affinity to protein kinase C, providing a f urther example of the application of carborane as the hydrophobic pharmacop hore of biologically active molecules. (C) 1999 Elsevier Science Ltd. All r ights reserved.