title: Protein kinase C modulators bearing dicarba-CLOSO-dodecaborane as a hydrophobic pharmacophore.
abstract: 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.
authors.affiliation: Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Endo
authors.forename: T
authors.initials: T
authors.lastname: Yoshimi
authors.forename: K
authors.initials: K
authors.lastname: Kimura
authors.forename: A
authors.initials: A
authors.lastname: Itai
mesh_terms: 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
chemical_list: D001896:Boron Compounds; D006574:Heterocyclic Compounds, 2-Ring; D011493:Protein Kinase C