Non-calcemic, antiproliferative, transcriptionally active...

Details Non-calcemic, antiproliferative, transcriptionally active... Non-calcemic, antiproliferative, transcriptionally active...

C - Chemistry, Metallurgy

07

C

C07C 401/00 (2006.01) A61K 31/59 (2006.01) A61K 31/593 (2006.01) A61P 3/02 (2006.01) A61P 17/08 (2006.01) A61P 35/00 (2006.01) A61P 43/00 (2006.01) C07C 313/04 (2006.01) C07C 317/08 (2006.01) C07J 9/00 (2006.01) C07B 53/00 (2006.01)

Patent

CA 2366586

Novel sulfur-containing analogs of 1.alpha.,25- dihydroxyvitamin D3 are provided. These analogs are synthesized in a convergent manner by joining A-ring and C,D ring fragments. Each analog with 1.alpha.,3.beta.-substituent stereochemistry shows a pharma- cologically desirable combination of high antiproliferative and high transcriptional activities in vitro and also low calcemic activity in vivo.

Cette invention concerne de nouveaux analogues renfermant du soufre, de 1 alpha ,25- dihydroxyvitamine D3. Ces analogues sont synthétisés de manière convergente par réunion de fragments de noyau A et de noyau C,D. Chaque analogue avec stéréochimie de substitution-1 DOLLAR (a)-3 beta présente une combinaison intéressante au plan pharmacologique de puissantes activités anti-prolifératives et transcriptionnelles in vitro, complétée par une faible activité calcémique in vivo.

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