AI Article Synopsis
- A series of new vitamin D3 analogues were created using a method called Negishi cross coupling, which combined specific zinc reagents with different aromatic compounds.
- The research focused on replacing part of the original vitamin D3 structure with a styrene unit to see how it would affect biological activity.
- The lead compound (compound 36) was found to be significantly less effective (12 times less) than calcitriol in promoting HL-60 cell differentiation, likely due to a reduced ability to bind to the vitamin D receptor (VDR).
Article Abstract
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.
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| http://dx.doi.org/10.1016/j.ejmech.2014.07.037 | DOI Listing |
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