School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Steroids. 2012 May;77(6):710-5. doi: 10.1016/j.steroids.2012.03.002. Epub 2012 Mar 14.
The preparation of steroidal[17,16-d][1,2,4]triazolo[1,5-a]pyrimidines and their biological evaluation as potential anticancer agents are herein reported. These novel heterosteroids (2, 4) were prepared through the condensation reaction of 3-amino-1,2,4-triazole with 16-arylidene-17-ketosteroids (1, 3). All the synthesized compounds were evaluated for their anticancer activity in vitro against PC-3 (human prostatic carcinoma), MCF-7 (human breast carcinoma) and EC9706 (human esophageal carcinoma) cell lines. Among the screened compounds, 2i, 2n and 4f showed significant inhibitory activity against all the three human cell lines.
本文报道了[17,16-d][1,2,4]三唑并[1,5-a]嘧啶甾体类化合物的制备及其作为潜在抗癌剂的生物评价。这些新型杂甾体（2,4）是通过 3-氨基-1,2,4-三唑与 16-亚芳基-17-酮甾体（1,3）的缩合反应制备的。所有合成的化合物均在体外对 PC-3（人前列腺癌）、MCF-7（人乳腺癌）和 EC9706（人食管癌）细胞系进行了抗癌活性评价。在所筛选的化合物中，2i、2n 和 4f 对所有三种人细胞系均表现出显著的抑制活性。
