Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids

Incorporation of zinc-binding groups into the side-chain of 1α,25-dihydroxyvitamin D3 (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.

Incorporation of zinc-binding groups into the side-chain of 1α,25-dihydroxyvitamin D3 (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.Figure optionsDownload as PowerPoint slide