Synthesis and in vitro cytotoxic activity evaluation of novel heterocycle bridged carbothioamide type isosteviol derivatives as antitumor agents

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• 作者：Song-Lin Zhu^a ; Ya Wu^a ; ^b ; Cong-Jun Liu^c ; Chang-Yong Wei^c ; Jing-Chao Tao^c ; ; Hong-Min Liu^a ; ^{liuhm@zzu.edu.cn}
• 关键词：Isosteviol ; Pyrazole ; Isoxazolidine ; Carbothioamide ; Cytotoxicity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：1 March, 2013
• 年：2013
• 卷：23
• 期：5
• 页码：1343-1346
• 全文大小：488 K

文摘

Two series of novel carbothioamide-substituted pyrazole and isoxazolidine derivatives were facilely prepared by functional interconversions in ring D of the tetracyclic diterpene isosteviol. The in vitro cytotoxic activities against four human tumor cell lines were evaluated. Our results indicated that carbothioamide-substituted pyrazole derivatives exhibited noteworthy cytotoxic activities. Specifically, compound 12p (IC₅₀ = 6.51 ¦ÌM) had the most potent cytotoxicity against Raji cell, which may be exploitable as a lead compound for the development of potent antitumor agents.