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Issue 24, 2003
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Remarkable effect of 2α-modification on the VDR antagonistic activity of 1α-hydroxyvitamin D3-26,23-lactones

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Abstract

Novel 2α-methyl-, 2α-(3-hydroxypropyl)- and 2α-(3-hydroxypropoxy)-substituted 25-dehydro-1α-hydroxyvitamin D3-26,23-lactone derivatives were efficiently synthesized via Reformatsky type allylation and palladium-catalyzed alkenylative cyclization processes, and their biological activities were evaluated. Introducing functional groups into the 2α-position of the vitamin D3-26,23-lactones resulted in remarkable enhancement of their antagonistic activity on vitamin D receptor (VDR).

Graphical abstract: Remarkable effect of 2α-modification on the VDR antagonistic activity of 1α-hydroxyvitamin D3-26,23-lactones

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Article information


Submitted
12 Sep 2003
Accepted
17 Oct 2003
First published
06 Nov 2003

Org. Biomol. Chem., 2003,1, 4396-4402
Article type
Paper

Remarkable effect of 2α-modification on the VDR antagonistic activity of 1α-hydroxyvitamin D3-26,23-lactones

N. Saito, T. Matsunaga, T. Fujishima, M. Anzai, H. Saito, K. Takenouchi, D. Miura, S. Ishizuka, H. Takayama and A. Kittaka, Org. Biomol. Chem., 2003, 1, 4396 DOI: 10.1039/B311107E

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