University Institute of Pharmaceutical Sciences, Sector-14, Panjab University, Chandigarh, India.
Arch Pharm (Weinheim). 2010 Jul;343(7):377-83. doi: 10.1002/ardp.200900258.
Varied positioning of the hydroximino group on the parental steroid skeleton results in remarkable changes in the antineoplastic activity profile of the compounds. Here, the compound 7-oximino-5-androstene and its O-alkylated derivatives have been prepared and screened for cytotoxic and aromatase inhibitory activity. The steroidal 7-oximino ether derivatives exhibited insignificant cytotoxic effects when screened against three cancer cell lines, MCF-7 (breast), NCl-H460 (lung), and SF-268 (CNS) at 100 microM. However, the imidazolyl-substituted steroidal oxime ethers displayed moderate inhibition of cytochrome P450 aromatase.
水肟基团在母体甾体骨架上的不同定位导致化合物的抗肿瘤活性谱发生显著变化。在这里，制备了化合物 7-肟基-5-雄烯及其 O-烷基化衍生物，并对其进行了细胞毒性和芳香酶抑制活性筛选。甾体 7-肟醚衍生物在 100μM 时对三种癌细胞系 MCF-7（乳腺）、NCl-H460（肺）和 SF-268（中枢神经系统）的细胞毒性作用不明显。然而，取代的咪唑基甾体肟醚显示出对细胞色素 P450 芳香酶的中等抑制作用。
