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This article is cited in 7 scientific papers (total in 7 papers)
Substituted androstanes as aromatase inhibitors
I. S. Levina N. D. Zelinskii Institute of Organic Chemistry
Abstract:
The synthesis and structure–activity relationships of inhibitors of steroid aromatase which catalyses the last stage of a multistep biotransformation of cholesterol into estrogens, viz., aromatisation of C19-steroids into C18-phenolic steroids, are discussed. Compounds of the androstane series which are structurally related to the natural substrate, viz., androst-4-ene-3,17-dione, are the subjects of consideration. The review encompasses problems of synthesis of various substituted androstanes and their aromatase-inhibiting activities and structural requirements for selective specific aromatase inhibitors based on in vitro and in vivo structure–activity studies of compounds synthesised, their biological properties and the results of clinical trials. Special attention is paid to practical applications of aromatase inhibitors in the treatment of hormone-dependent mammary and ovarian tumours as well as benign prostatic tumours. In writing this report, the author has used all the information currently available in the chemical, biochemical, endocrinological and medicinal literature as well as in patents. The bibliography includes 173 references.
Received: 03.10.1997
Citation:
I. S. Levina, “Substituted androstanes as aromatase inhibitors”, Usp. Khim., 67:11 (1998), 1068–1093; Russian Chem. Reviews, 67:11 (1998), 975–998
Linking options:
https://www.mathnet.ru/eng/rcr1436https://doi.org/10.1070/RC1998v067n11ABEH000427 https://www.mathnet.ru/eng/rcr/v67/i11/p1068
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