Low-Calcemic, Highly Antiproliferative, 1-Difluoromethyl Hybrid Analogs of the Natural Hormone 1α,25-Dihydroxyvitamin D3:  Design, Synthesis, and Preliminary Biological Evaluation

Low-Calcemic, Highly Antiproliferative, 1-Difluoromethyl Hybrid Analogs of the Natural Hormone 1α,25-Dihydroxyvitamin D3:  Design, Synthesis, and Preliminary Biological Evaluation

Replacing the 1α-OH group of the natural hormone 1α,25-dihydroxyvitamin D3 (calcitriol) by a 1α-CHF2 group and incorporating a potentiating side chain produced two new hybrid analogs 6 and 7. Both of these two hybrid analogs are as transcriptionally active as calcitriol and are strongly antiprolifer...

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Veröffentlicht in:Journal of medicinal chemistry 2006-12, Vol.49 (25), p.7513-7517
Hauptverfasser: Peleg, Sara, Petersen, Kimberly S, Suh, Byung Chul, Dolan, Patrick, Agoston, Elin S, Kensler, Thomas W, Posner, Gary H
Format: Artikel
Sprache:eng
Schlagworte:
Antineoplastic agents
Biological and medical sciences
General aspects
Medical sciences
Pharmacology. Drug treatments
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Zusammenfassung:Replacing the 1α-OH group of the natural hormone 1α,25-dihydroxyvitamin D3 (calcitriol) by a 1α-CHF2 group and incorporating a potentiating side chain produced two new hybrid analogs 6 and 7. Both of these two hybrid analogs are as transcriptionally active as calcitriol and are strongly antiproliferative in vitro but are low-calcemic in vivo.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm0609925