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17-位杂环取代的雄烯衍生物可以作为人细胞色素P450_17α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P45017(酶有较好的抑制作用, IC50 为225 nmol·L-1。
17-Heterocyclic substituted androstene derivatives can be used as effective inhibitors of human cytochrome P450 17α enzyme to inhibit the androgen biosynthesis in vivo and have a good application prospect in the treatment of benign prostatic hyperplasia (BPH) and prostate cancer. Seven novel 17 - [(2’-substituted) -4’-pyrimidinyl] androstene derivatives were designed and synthesized. Their structures were confirmed by 1H NMR, IR and elemental analysis or MS spectra. The pharmacological activities of the compounds showed that the compound 5 had a good inhibitory effect on P45017 (IC50: 225 nmol·L-1).