2. Academic Validation
  3. Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation

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

  • J Med Chem. 2006 Dec 14;49(25):7513-7. doi: 10.1021/jm0609925.
Sara Peleg 1,  Kimberly S Petersen,  Byung Chul Suh,  Patrick Dolan,  Elin S Agoston,  Thomas W Kensler,  Gary H Posner
Affiliations

Affiliation

  • 1 Department of Endocrine Neoplasia and Hormonal Disorders, The University of Texas, M.D. Anderson Cancer Center, Houston, Texas 77030, USA.
PMID: 17149880 DOI: 10.1021/jm0609925
Abstract

Replacing the 1alpha-OH group of the natural hormone 1alpha,25-dihydroxyvitamin D(3) (calcitriol) by a 1alpha-CHF(2) 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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