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

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.

journal_name

J Med Chem

authors

Peleg S,Petersen KS,Suh BC,Dolan P,Agoston ES,Kensler TW,Posner GH

doi

10.1021/jm0609925

subject

Has Abstract

pub_date

2006-12-14 00:00:00

pages

7513-7

issue

25

eissn

0022-2623

issn

1520-4804

journal_volume

49

pub_type

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