期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 86, 期 -, 页码 381-393出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.07.037
关键词
Aromatic analogues of vitamin D3; Negishi coupling reaction; Antiproliferative activity
资金
- Les Laboratoires Servier
In an effort to develop novel vitamin D3 analogues, a series of aromatic compounds was synthetized, using efficient Negishi cross coupling between alkenylzinc reagents of the C,D-ring moiety of vitamin D3, and various substituted aromatic halides as A-ring mimics. The study aimed at exploring the influence of the replacement of the original vitamin D3 diene by a styrene unit on the biological activities. Potency in the induction of the differentiation of HL-60 cells for the lead compound 36 was 12 fold less important than calcitriol correlating with a weaker binding affinity for VDR. (C) 2014 Elsevier Masson SAS. All rights reserved.
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