non calcemische, transkriptionell - active sulphur containing analogues of 1 alpha, 25 dihydroxyvitamin d3 with antiproliferative effect

摘要

Novel sulfur-containing analogs of 1±,25-dihydroxyvitamin D 3 are provided. These analogs are synthesized in a convergent manner by joining A-ring and C,D ring fragments. Each analog with 1±,3²-substituent stereochemistry shows a pharmacologically desirable combination of high antiproliferative and high transcriptional activities in vitro and also low calcemic activity in vivo.