Polymethylcarborane as a novel bioactive moiety: derivatives with potent retinoid antagonistic activity.
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.
Endo
Y
Y
Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan. yendo@mol.f.u-tokyo.ac.jp
Yaguchi
K
K
Kawachi
E
E
Kagechika
H
H
D001565:Benzoates / Q000737:chemistry / Q000494:pharmacology*; D001896:Boron Compounds / Q000737:chemistry / Q000494:pharmacology*; D002454:Cell Differentiation / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D012176:Retinoids / Q000037:antagonists & inhibitors*
C416355:4-((deca-B-methyl-1,12-dicarba-closo-dodecaboran-1-yl)carbamoyl)benzoic acid; D001565:Benzoates; D001896:Boron Compounds; D012176:Retinoids