The Effect of Exchanging Various Substituents at the 2-Position of 2-Methoxyestradiol on Cytotoxicity in Human Cancer Cell Cultures and Inhibition of Tubulin Polymerization

A new set of estradiol derivatives bearing various substituents at the 2-position were synthesized in order to further elucidate the structural parameters associated with the antitubulin activity and cytotoxicity of 2-substituted estradiols

Mark Cushman

2002

Scholarcy highlights

  • A new set of estradiol derivatives bearing various substituents at the 2-position were synthesized in order to further elucidate the structural parameters associated with the antitubulin activity and cytotoxicity of 2-substituted estradiols
  • The substituents introduced into the 2-position of estradiol included E-3‘-hydroxy-1‘-propenyl, 2‘-hydroxyethoxy, 3-N,N-dimethylaminoethylideneamino, 2‘-hydroxyethylineneamino,ethenyl, phenylethynyl, ethynly, 1‘-propynyl, and cyano
  • The remaining compounds were all inactive as inhibitors of tubulin polymerization when tested at concentrations of up to 40 μM
  • All of the compounds were cytotoxic in a panel of 55 human cancer cell cultures, and in general, the most cytotoxic compounds were the most potent as inhibitors of tubulin polymerization. 2-(1‘-Propynyl)estradiol displayed significant anticancer activity in the in vivo hollow fiber animal model

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