Abstract
Eight new side-chain allylic, benzylic, and propargylic ether analogs of the natural hormone calcitriol have been rationally designed and easily synthesized. Three of these 23-oxa ether analogs lacking the typical side-chain OH group are more antiproliferative in vitro and desirably less calcemic in vivo than the natural hormone. One of these three 23-oxa analogs has transcriptional potency almost as high as that of calcitriol, even though it binds to the human vitamin D receptor only about 1% as well as calcitriol.
Original language | English (US) |
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Pages (from-to) | 5824-5832 |
Number of pages | 9 |
Journal | Journal of medicinal chemistry |
Volume | 50 |
Issue number | 23 |
DOIs | |
State | Published - Nov 15 2007 |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery