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Human Reproduction, Vol. 9, No. suppl_1, pp. 32-39, 1994
© 1994 European Society of Human Reproduction and Embryology

Effects of D-ring substituents on antiprogestational (antagonist) and progestational (agonist) activity of 11β-aryl steroids

C.E. Cook, Y.-W. Lee, M.C. Wani, P.A. Fail and V. Petrow

Research Triangle Institute P.O. Box 12194, Research Triangle Park, NC 27709-2194, USA

The discovery of antiprogestational steroids by the Roussel-Uclaf group not only was a major scientific advance but also opened the way to new methods of fertility control and new therapies for such conditions as cancer. RU486, the prototype of the series, is distinguished by a p (N,N-dlmethylaminophenyl) substituent at the 11β- position of the steroid framework, a 4,9-dien-3-one system and 17β-hydroxy-17{alpha}-propynyl substituents. We examined the effect of varying the 17{alpha}- substituent in 17β-hydroxy compounds analogous to RU486, the effect of introducing a progesterone side chain at C-17, and the effects of further substitution at C-17{alpha} and C-16{alpha}on the activity of these latter compounds. These studies indicate an important role for D-ring substituents in determining the balance of agonist/antagonist activity in this series. For example, l7{alpha}-acetoxy-17β-acetyl substitution gave a potent antagonist, whereas 16{alpha}-ethyl-17β-acetyl substitution resulted in a compound with potent progestational (agonist) activity. The compounds present opportunities for further interesting and useful biological investigations.

Key words: activity/antiprogestins/progestins/receptor binding/synthesis


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