Polymethylcarborane as a novel bioactive moiety: derivatives with potent retinoid antagonistic activity

Bioorg Med Chem Lett. 2000 Aug 7;10(15):1733-6. doi: 10.1016/s0960-894x(00)00327-9.

Abstract

4[(Deca-B-methyl-1,12-dicarba-closo-dodecaboran-1-yl)c arbamoyl]benzoic acid and its congeners showed potent antagonistic activity at concentrations of 10(-7)-10(-8) M on the differentiation-inducing action of retinoids towards human promyelocytic leukemia HL-60 cells. This is the first example of derivatives of polymethylcarborane, which resembles C60 in size, with biological activity.

MeSH terms

  • Benzoates / chemistry
  • Benzoates / pharmacology*
  • Boron Compounds / chemistry
  • Boron Compounds / pharmacology*
  • Cell Differentiation / drug effects
  • HL-60 Cells
  • Humans
  • Retinoids / antagonists & inhibitors*

Substances

  • 4-((deca-B-methyl-1,12-dicarba-closo-dodecaboran-1-yl)carbamoyl)benzoic acid
  • Benzoates
  • Boron Compounds
  • Retinoids