Synthesis and bioevaluation of novel steroidal isatin conjugates derived from epiandrosterone/androsterone. (1st January 2019)

• Record Type: Journal Article
• Authors: Ke, Shaoyong; Zhang, Zhigang; Liu, Manli; Fang, Wei; Huang, Daye; Wan, Zhongyi; Zhou, Ronghua; Wang, Kaimei; Shi, Liqiao
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 34:Number 1(2019)
• Page Start: 1607
• Page End: 1614
• Publication Date: 2019-01-01
• Subjects: Epiandrosterone -- androsterone -- isatin -- conjugate -- synthesis -- cytotoxic activity; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.1080/14756366.2019.1659790
• Languages: English
• ISSNs: 1475-6366

Abstract

Abstract: 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.