Department of Chemistry, McGill University, Montreal, QC, Canada.
Bioorg Med Chem. 2010 Jun 1;18(11):4119-37. doi: 10.1016/j.bmc.2010.03.078. Epub 2010 Apr 7.
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.
将锌结合基团整合到 1α,25-二羟维生素 D（3）（1,25D）的侧链中，形成具有双重功能的杂合分子，既能作为维生素 D 受体激动剂，又能作为组蛋白去乙酰化酶抑制剂。这些双功能杂合体在体外对 AT84 鳞状癌细胞系表现出抗增殖活性，而没有 1,25D 的体内高钙血症作用。
