Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids

Bioorg Med Chem. 2010 Jun 1;18(11):4119-37. doi: 10.1016/j.bmc.2010.03.078. Epub 2010 Apr 7.

Abstract

Incorporation of zinc-binding groups into the side-chain of 1alpha,25-dihydroxyvitamin D(3) (1,25D) fully bifunctional hybrid molecules which act both as vitamin D receptor agonists and histone deacetylase inhibitors. These bifunctional hybrids display in vitro antiproliferative activity against the AT84 squamous carcinoma cell line while lacking the in vivo hypercalcemic effects of 1,25D.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Carcinoma, Squamous Cell / drug therapy
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Histone Deacetylase Inhibitors / chemistry*
  • Humans
  • Receptors, Calcitriol / agonists*
  • Vitamin D / analogs & derivatives*
  • Vitamin D / chemistry
  • Zinc / chemistry*

Substances

  • Antineoplastic Agents
  • Histone Deacetylase Inhibitors
  • Receptors, Calcitriol
  • dihydroxy-vitamin D3
  • Vitamin D
  • Zinc