Laura Sánchez-Abella et al.
Journal of medicinal chemistry, 52(19), 6158-6162 (2009-09-11)
We have synthesized several isomers of 19-nor-vitamin D analogues possessing a hydroxy group at C-2 as well as novel derivatives bearing an epoxy substituent at the A-ring. All vitamins were prepared in convergent syntheses utilizing the modified Julia olefination. 1alpha,2alpha,25-Trihydroxy-19-nor-vitamin...
Convergent synthesis of double point modified analogs of 1α, 25-dihydroxyvitamin D2 for biological evaluation
Nadkarni S, et al.
The Journal of Steroid Biochemistry and Molecular Biology, 164, 45-49 (2016)
Yuka Inaba et al.
Journal of medicinal chemistry, 52(5), 1438-1449 (2009-02-06)
To identify novel vitamin D receptor (VDR) ligands that induce a novel architecture within the ligand-binding pocket (LBP), we have investigated eight 22-butyl-1alpha,24-dihydroxyvitamin D(3) derivatives (3-10), all having a butyl group as the branched alkyl side chain. We found that...
Masato Shimizu et al.
Bioorganic & medicinal chemistry, 16(14), 6949-6964 (2008-06-10)
Recently, we have found that 16-ene-22-thia-26,27-dimethyl-19-norvitamin D(3) analogs 1a (n=2, 3) are 20 times more active than the natural hormone 1alpha,25-dihydroxyvitamin D(3) in terms of transcriptional activity. To further investigate the effects of the A-ring modification of 1a, b on...
Marc Lamblin et al.
Bioorganic & medicinal chemistry, 18(11), 4119-4137 (2010-05-11)
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...