Protein kinase C modulators bearing dicarba-CLOSO-dodecaborane as a hydrophobic pharmacophore.
The size and position of a hydrophobic moiety on a benzolactam skeleton, which reproduces the active conformation and biological activity of teleocidins, play an important role in the appearance of the activity. We have designed and synthesized benzolactams bearing dicarba-closo-dodecaborane. These compounds showed potent binding affinity to protein kinase C, providing a further example of the application of carborane as the hydrophobic pharmacophore of biologically active molecules.
Endo
Y
Y
Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan.
Yoshimi
T
T
Kimura
K
K
Itai
A
A
D001896:Boron Compounds / Q000737:chemistry*; D006574:Heterocyclic Compounds, 2-Ring / Q000737:chemistry*; D008958:Models, Molecular; D011485:Protein Binding; D011493:Protein Kinase C / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship
D001896:Boron Compounds; D006574:Heterocyclic Compounds, 2-Ring; D011493:Protein Kinase C