Abstract
A series 5-8 of 1- and 3-CH2OH 19-nor analogs of the hormone calcitriol (1) has been prepared. Surprisingly, 19-nor 1α-CH2OH analog 5a is more antiproliferative at 100 nM concentration than the corresponding regioisomeric analog 6a with the natural 1α-OH group, and 1α-CH2OH hybrid analog 7a is similar in antiproliferative potency to calcitriol (1) even at low nanomolar concentrations.
Original language | English (US) |
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Pages (from-to) | 3964-3976 |
Number of pages | 13 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 13 |
Issue number | 12 |
DOIs | |
State | Published - Jun 2 2005 |
Keywords
- 19-Nor
- Calcitriol
- Hydroxymethyl A-ring
- Novel analogs
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry