- Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
Bioorganic & medicinal chemistry (2010-05-11)
Marc Lamblin, Basel Dabbas, Russell Spingarn, Rodrigo Mendoza-Sanchez, Tian-Tian Wang, Beum-Soo An, Dao Chao Huang, Richard Kremer, John H White, James L Gleason
PMID20452225
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.