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.
Highlights
Cancer is the second cause of death in the world, which denotes a real crisis for public health in the worldwide with the ecological changes and environmental deterioration[1,2,3]
Steroids are classes of natural products widely distributed in plants, beverages, wellcooked foods and tobacco smoke and with special four-ring structural features, which have been demonstrated to exhibit broad biological functions, and have attracted increasing interest from bioorganic and pharmaceutical researches[12,13,14]
Isatin is a natural indole alkaloid consisted in a number of plants, which has been found to be a common scaffold in various drugs, agrochemicals, and dyes[15,16,17,18]
Summary
Cancer is the second cause of death in the world, which denotes a real crisis for public health in the worldwide with the ecological changes and environmental deterioration[1,2,3]. A series of novel steroid-isatin conjugates 3a–h and 6a–h were designed and synthesized as shown in Scheme 1, and their potential inhibition on three cell lines (SGC-7901, A875, HepG2) were evaluated by MTT (3–(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) colorimetric method, and the possible structure-activity relationships have been summarized and discussed. According to the results shown, most of these steroidal isatin derivatives 3a–h and 6a–h present good cytotoxic activities (75–85%) against the tested cell lines compared with the control at the concentration of 20 mg/mL. These results can further confirm the cytotoxic activity of these steroidal isatin derivatives are highly potential scaffold to discovery of potential anti-cancer agents.
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