Synthesis and bioevaluation of novel steroidal isatin conjugates derived from epiandrosterone/androsterone
文献类型： 外文期刊
作者： Ke, Shaoyong 1 ; Zhang, Zhigang 1 ; Liu, Manli 1 ; Fang, Wei 1 ; Huang, Daye 1 ; Wan, Zhongyi 1 ; Zhou, Ronghua 1 ; Wang, 1 ;
作者机构： 1.Hubei Acad Agr Sci, Natl Biopesticide Engn Res Ctr, Hubei Biopesticide Engn Res Ctr, Wuhan 430064, Hubei, Peoples R China
关键词： Epiandrosterone; androsterone; isatin; conjugate; synthesis; cytotoxic activity
期刊名称：JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY （ 影响因子：5.051； 五年影响因子：4.598 ）
ISSN： 1475-6366
年卷期： 2019 年 34 卷 1 期
页码：
收录情况： SCI
摘要： Steroids are classes of natural products widely distributed in nature, which have been demonstrated to exhibit broad biological functions, and have also attracted increasing interest from bioorganic and pharmaceutical researches. In order to develop novel chemical entities as potential cytotoxic agents, a series of steroidal isatin conjugations derived from epiandrosterone and androsterone were efficiently prepared and characterized, and all these obtained compounds were screened for their potential cytotoxic activities. The preliminary bioassay indicated that most of the newly synthesized compounds exhibited good cytotoxic activities against human gastric cancer (SGC-7901), melanoma (A875), and hepatocellular liver carcinoma (HepG2) cell lines compared with 5-fluorouracil (5-FU), which might be considered as promising scaffold for further development of potential anticancer agents.
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