Synthesis and bioevaluation of novel steroidal isatin conjugates derived from epiandrosterone/androsterone

• Main Authors: Shaoyong Ke, Zhigang Zhang, Manli Liu, Wei Fang, Daye Huang, Zhongyi Wan, Ronghua Zhou, Kaimei Wang, Liqiao Shi
• Format: Article
• Language: English
• Published: Taylor & Francis Group 2019-01-01
• Series: Journal of Enzyme Inhibition and Medicinal Chemistry
• Subjects: epiandrosterone; androsterone; isatin; conjugate; synthesis; cytotoxic activity
• Online Access: http://dx.doi.org/10.1080/14756366.2019.1659790

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.