Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1α,25-dihydroxyvitamin D3: Design, synthesis, and preliminary biological evaluation

Sara Peleg; Kimberly S. Petersen; Byung Chul Suh; Patrick Dolan; Elin S. Agoston; Thomas W. Kensler; Gary H. Posner

doi:10.1021/jm0609925

Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1α,25-dihydroxyvitamin D₃: Design, synthesis, and preliminary biological evaluation

Sara Peleg, Kimberly S. Petersen, Byung Chul Suh, Patrick Dolan, Elin S. Agoston, Thomas W. Kensler, Gary H. Posner

Bloomberg School of Public Health

Research output: Contribution to journal › Article › peer-review

16 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	7513-7517
Number of pages	5
Journal	Journal of medicinal chemistry
Volume	49
Issue number	25
DOIs	https://doi.org/10.1021/jm0609925
State	Published - Dec 14 2006

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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10.1021/jm0609925

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Peleg, S., Petersen, K. S., Suh, B. C., Dolan, P., Agoston, E. S., Kensler, T. W., & Posner, G. H. (2006). Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1α,25-dihydroxyvitamin D₃: Design, synthesis, and preliminary biological evaluation. Journal of medicinal chemistry, 49(25), 7513-7517. https://doi.org/10.1021/jm0609925

Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1α,25-dihydroxyvitamin D₃: Design, synthesis, and preliminary biological evaluation. / Peleg, Sara; Petersen, Kimberly S.; Suh, Byung Chul et al.
In: Journal of medicinal chemistry, Vol. 49, No. 25, 14.12.2006, p. 7513-7517.

Research output: Contribution to journal › Article › peer-review

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abstract = "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.",

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AU - Kensler, Thomas W.

AU - Posner, Gary H.

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Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1α,25-dihydroxyvitamin D₃: Design, synthesis, and preliminary biological evaluation

Abstract

ASJC Scopus subject areas

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