YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
17-Deoxysteroid類の合成と抗男性ホルモン作用
舛岡 豊増岡 通夫後藤 義一平賀 謙太郎中山 亮三木 卓一角 正夫
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1983 年 103 巻 10 号 p. 1046-1053

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On the basis of the mechanism of action of new antiandrogens, 16β-alkyltestosterones (1) and 16β-alkyl-19-nortestosterones (2), we designed and synthesized a series of 17-deoxyandrost-4-en-3-ones (12-14, 16, and 19) having substituent (s) at C-1, C-6, and C-7 positions and 17-deoxy-16β-alkylestr-4-en-3-ones (6) together with 17-deoxytestosterone (7) and 17-deoxy-19-nortestosterone (6 : R=H). The antiandrogenic activity was determined using immature orchiectomized rats treated with testosterone propionate. These compounds except 6 were found to show considerable antiandrogenic activity by subcutaneous or oral administration. The biological result means that 17β-hydroxyl group on the steroids was not indispensable for the manifestation of antiandrogenic activity. A new formylation reaction using orthoformate-boron trifluoride etherate instead of Vilsmeier reagent was described for the preparation of 6-formyltestosterone derivatives (9 and 22)

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