Synthesis and anti-tumor activity of new steroidal nuclear analogues of aragusterol A
Hidemichi Mitome1, Masakazu Shinohara, Hiroaki Miyaoka
1School of Pharmacy, Tokyo University of Pharmacy and Life Science, Tokyo, Japan.
Abstract:
3alpha,7alpha-Dihydroxy-5-epiaragusterol A (3) was synthesized from bile acid (cholic acid) as a new steroidal nuclear analogue of antitumor marine steroid aragusterol A. 7alpha-Hydroxyaragusterol A (4) was also derived from xestokerol B. The in vitro anti-proliferative activity of each of these analogues toward KB cells as well as in vivo anti-tumor activity of 5-epiaragusterol A (2) previously synthesized by the authors and 3 were assessed.
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