synthesis and 5α-reductase inhibitory activity of c21 steroids having 1,4-diene or 4,6-diene 20-ones and 4-azasteroid 20-oximes合成和5α-reductase c21类固醇抑制活动1,4-diene或4,6-diene 20例和4-azasteroid 20-oximes.pdfVIP

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synthesis and 5α-reductase inhibitory activity of c21 steroids having 1,4-diene or 4,6-diene 20-ones and 4-azasteroid 20-oximes合成和5α-reductase c21类固醇抑制活动1,4-diene或4,6-diene 20例和4-azasteroid 20-oximes.pdf

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synthesis and 5α-reductase inhibitory activity of c21 steroids having 1,4-diene or 4,6-diene 20-ones and 4-azasteroid 20-oximes合成和5α-reductase c21类固醇抑制活动1,4-diene或4,6-diene 20例和4-azasteroid 20-oximes

Molecules 2012, 17, 355-368; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis and 5α-Reductase Inhibitory Activity of C21 Steroids Having 1,4-diene or 4,6-diene 20-ones and 4-Azasteroid 20-Oximes Sujeong Kim 1, Yong-ung Kim 2,* and Eunsook Ma 1,* 1 College of Pharmacy, Catholic University of Daegu, Hayang, 712-702, Korea 2 College of Herbal Bio-industry, Daegu Hany University, Gyeongsangbuk-do 712-715, Korea * Authors to whom correspondence should be addressed; E-Mails: ykim@dhu.ac.kr (Y.-U.K.); masook@cu.ac.kr (E.M.); Tel.: Tel. +82-53-819-1404 (Y.-U.K.); +82-53-850-3621 (E.M.); Fax: Fax: +82-53-819-1272 (Y.-U.K.); +82-53-850-3602(E.M.). Received: 1 November 2011; in revised form: 14 December 2011 / Accepted: 16 December 2011 / Published: 30 December 2011 Abstract: The synthesis and evaluation of 5α-reductase inhibitory activity of some 4-azasteroid-20-ones and 20-oximes and 3β-hydroxy-, 3β-acetoxy-, or epoxy-substituted C21 steroidal 20-ones and 20-oximes having double bonds in the A and/or B ring are described. Inhibitory activity of synthesized compounds was assessed using 5α-reductase enzyme and [1,2,6,7-3H]testosterone as substrate. All synthesized compounds were less active than finasteride (IC50 : 1.2 nM). Three 4-azasteroid-2-oximes (compounds 4, 6 and 8) showed good inhibitory activity (IC50 : 26, 10 and 11 nM) and were more active than corresponding 4-azaster