(20R) and (20S)-24-(p-toluenesulfonyloxy)-25,26,27-trinorvitamin D₃ analogs and their uses

摘要

This invention discloses (20R) and (20S)-24-(p-toluenesulfonyloxy)-25,26,27-trinorvitamin D₃ analogs, and especially (20R)-25,26,27-trinor-24-(p-methylphenylsulfonate)-vitamin D₃, its biological activities, and pharmaceutical uses therefor. This compound exhibits relatively little calcemic activity and does not promote cellular differentiation of HL-60 leukemia cells, but rather kills the cells. This cell death activity is found in small cell lung carcinoma also, but not in prostate, bone or ovarian cancer cells. This compound thus causes specific cell death in the absence of changes in calcium levels and without general toxicity in an animal. Therefore it might serve as a useful therapy for treatment of some forms of cancer, such as leukemia and lung cancer.