Systematic SAR study of the side chain of nonsecosteroidal vitamin D3 analogs.
Bioorg Med Chem
; 20(14): 4495-506, 2012 Jul 15.
Article
em En
| MEDLINE
| ID: mdl-22677528
ABSTRACT
A series of nonsecosteroidal vitamin D(3) analogs with carboxylic acid were explored. Through our systematic SAR studies on the side chain moiety, compound 6b was identified as the optimal compound showing excellent vitamin D receptor (VDR) agonistic activity. Compound 6b had the diethyl group in the terminal which was bound by (E)-olefin linker to the bisphenyl core. Calculating the volume of the side chain showed that the diethyl group in 6b filled the hydrophobic region of VDR with the ideal packing coefficient based on the 55% rule, and that this resulted in the most potent in vitro activity.
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1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Calcitriol
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article