Non-calcemic, antiproliferative, transcriptionally active 24-flu

Details Non-calcemic, antiproliferative, transcriptionally active 24-flu Non-calcemic, antiproliferative, transcriptionally active 24-flu

1999-06-01

2000-03-28

Dees, Jose C.

Organic compounds -- part of the class 532-570 series

Organic compounds

9,10-seco-cyclopentanohydrophenanthrene ring system or...

552653, 514167, C07C40100, A61K 3159

Patent

active

060433868

ABSTRACT:
Fluorinated analogs of 1.alpha.,25-dihydroxyvitamin D.sub.3. These analogs are synthesized in a convergent manner by joining A-ring and C,D-ring fragments. Each hybrid analog, having a calcemia-lowering 1-hydroxymethyl group and a potentiating 16-ene-24,24-difluorinated C,D-ring and side chain, is designed to be lipophilic and inert toward 24-hydroxylase enzyme catabolism. Each hybrid analog with 1.beta.,3.alpha.-substituent stereochemistry shows a pharmacologically desirable combination of high antiproliferative and high transcriptional activities in vitro and also low calcemic activity in vivo.

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patent: 5830885 (1998-11-01), Posner
Vanham et al. (J. Steroid Chem. Biochem. (1988), 29(4), 381-6), 1988.

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