Department of Chemistry, Islamia College of Science and Commerce, Srinagar 190009, India.
Steroids. 2010 Dec;75(12):801-4. doi: 10.1016/j.steroids.2010.02.015. Epub 2010 Mar 4.
A facile synthesis of 21-triazolyl derivatives of pregnenolone and their potential antitumour activity is reported. The scheme involves the transformation of the starting pregnenolone acetate into pregnenolone, conversion of pregnenolone to 21-bromo pregnenolone and finally the one-pot, two-step in situ conversion of the bromo derivative to the 21-triazolyl pregnenolone using the 'click chemistry' approach. These derivatives were screened for their anticancer activity against seven human cancer cell lines. The compounds especially 5a, 5b, 5c, 5e, 5g and 5h exhibited significant anticancer activity with compound 5e as the most active in this study.
报道了一种简便的孕烯醇酮 21-三唑衍生物的合成方法及其潜在的抗肿瘤活性。该方案包括将起始孕烯醇酮醋酸酯转化为孕烯醇酮，将孕烯醇酮转化为 21-溴孕烯醇酮，最后使用“点击化学”方法将溴代衍生物一锅两步原位转化为 21-三唑基孕烯醇酮。这些衍生物被筛选用于对七种人癌细胞系的抗癌活性。特别是化合物 5a、5b、5c、5e、5g 和 5h 表现出显著的抗癌活性，其中化合物 5e 在本研究中最为活跃。
