CAJ | 학술논문

17-位杂环取代的雄烯衍生物可以作为人细胞色素P45017α酶的有效抑制剂,抑制体内雄激素的生物合成,在治疗良性前列腺增生(BPH)和前列腺癌方面有良好的应用前景.设计并合成了七个新的17-[(2＇-取代的)-4＇-嘧啶基]雄烯衍生物,化合物的结构经1H NMR、IR和元素分析或MS谱确证.化合物的药理活性实验结果表明,化合物5对P45017α酶有较好的抑制作用,IC50为225 nmo1@L-1.
17-위잡배취대적웅희연생물가이작위인세포색소P45017α매적유효억제제,억제체내웅격소적생물합성,재치료량성전렬선증생(BPH)화전렬선암방면유량호적응용전경.설계병합성료칠개신적17-[(2＇-취대적)-4＇-밀정기]웅희연생물,화합물적결구경1H NMR、IR화원소분석혹MS보학증.화합물적약리활성실험결과표명,화합물5대P45017α매유교호적억제작용,IC50위225 nmo1@L-1.
17-Heterocyclic substituted androstene derivatives have been found to be potent innibitors forhuman testicular microsomal 17α-hydroxylase/C17,20-layse, which have potential usage in the treatment of benignprostatic hypertrophy(BPH) and prostatic cancer. In order to further investigate their structure-activity relationships,the compounds were confirmed by IR, 1H NMR, elemental analysis or MS measurements. The results of thepharmacological activity tests showed that°compound 5 is a potent inhibitor for P45017α with IC50 225 nmol@L-1.