Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
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.
Lamblin
Marc
M
Department of Chemistry, McGill University, Montreal, QC, Canada.
Dabbas
Basel
B
Spingarn
Russell
R
Mendoza-Sanchez
Rodrigo
R
Wang
Tian-Tian
TT
An
Beum-Soo
BS
Huang
Dao Chao
DC
Kremer
Richard
R
White
John H
JH
Gleason
James L
JL
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D002294:Carcinoma, Squamous Cell / Q000188:drug therapy; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D056572:Histone Deacetylase Inhibitors / Q000737:chemistry*; D006801:Humans; D018167:Receptors, Calcitriol / Q000819:agonists*; D014807:Vitamin D / Q000031:analogs & derivatives* / Q000737:chemistry; D015032:Zinc / Q000737:chemistry*
D000970:Antineoplastic Agents; D056572:Histone Deacetylase Inhibitors; D018167:Receptors, Calcitriol; C118756:dihydroxy-vitamin D3; D014807:Vitamin D; D015032:Zinc