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

Research output: Contribution to journalArticle

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 languageEnglish (US)
Pages (from-to)7513-7517
Number of pages5
JournalJournal of medicinal chemistry
Volume49
Issue number25
DOIs
StatePublished - Dec 14 2006

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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