76763-14-9Relevant articles and documents
Anti-AIDS agents. Part 36: 17-carboxylated steroids as potential anti-HIV agents
Xia, Peng,Yang, Zheng-Yu,Xia, Yi,Zheng, Yun-Qing,Cosentino, L.Mark,Lee, Kuo-Hsiung
, p. 1907 - 1911 (1999)
In our search for novel anti-HIV agents, seven 17-carboxylated steroid derivatives were synthesized and evaluated as potential anti-HIV agents. Compound 13 exhibited potent anti-HIV activity in acutely infected H9 lymphocytes with EC50 and therapeutic index values of 0.8 μM and 300, respectively.
Synthesis and bioactivity of new Finasteride conjugate
Shuang, Zhao,Jiazhen, Wu,Lijuan, Yang,Zhuo, Li,Dahai, Yu,Jinfeng, Li,Jing, Yu,Yongtao, Liang,En-Si, Wang,Xuexun, Fang
supporting information; experimental part, p. 3439 - 3442 (2011/07/07)
Finasteride is a synthetic 4-azasteroid compound that acts by inhibiting type II 5α-reductase, the enzyme that converts the androgen testosterone to 5α-dihydrotestosterone. It was approved by the US FDA for the treatment of benign prostatic hyperplasia and male pattern baldness. Here the acylation product of Finasteride C-18 amide N-polimod was synthesized by employing acylation reaction with polimod amide as a pivotal intermediate. The structure of the key intermediate and target molecule was confirmed by infrared spectrum, 1H NMR and 13C NMR spectra and mass spectrum, and the inhibition of the steroid 5α-reductase and the rats' benign prostatic hyperplasia by the new Finasteride conjugate and Finasteride was also determined. The inhibition of the Finasteride conjugate on 5α-reductase was stronger than that of Finasteride. Prostate hyperplasia of rats was reduced by Finasteride conjugate treatment similar to the Finasteride treatment. However, the Finasteride conjugate treated animals showed better viable condition than the Finasteride treated ones, suggesting the new compound may have improved toxicity profile than Finasteride.
METHOD FOR THE SELECTIVE PREPARATION OF 3-OXO-4-AZA-5A-ANDROSTANE COMPOUND
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Page 5, (2008/06/13)
This invention relates to a method for selectively preparing the 3-oxo-4-aza-5¥á-androstane compound which is used as an intermediate of finasteride by heating 3-oxo-4-aza-5-androstene in a mixture of formic acid and an alkanediol in the presence of zinc.