Preparations of Heterospirostanols and Their Pharmacological Activities.

Abstract

Steroids Steroids U 0300Preparations of Heterospirostanols and Their Pharmacological Activities. -Heterospirostanol derivatives bearing sulfur and selenium atoms as well as oxygen and nitrogen atoms on the F-ring are prepared by using 26-iodopseudodiosgenin as a key intermediate. The pharmacological behavior of the derivatives with respect to the inhibition of interferon-γ production, cytotoxic activities, antiurease activities, and antibacterial activities is examined. Compounds (I) exhibit inhibitory activity against interferon-γ production while spirostanols (Ia) and (II) and pseudo derivative (III) show activity against cancerous HCT 116 cells. In addition, pseudo derivatives (III) and (IV) bearing a cyanoseleno group at C-26 provide antiurease and antibacterial activities. -(QUAN, H.-J.; KOYANAGI, J.; OHMORI, K.; UESATO, S.; TSUCHIDO, T.; SAITO*, S.; Eur.