Synthesis of novel 2-cyano substituted glycyrrhetinic acid derivatives as inhibitors of cancer cells growth and NO production in LPS-activated J-774 cells

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• 作者：Oksana V. Salomatina ; Andrey V. Markov ; Evgeniya B. Logashenko ; Dina V. Korchagina ; Marina A. Zenkova ; Nariman F. Salakhutdinov ; Valentin V. Vlassov ; Genrikh A. Tolstikov
• 关键词：Glycyrrhetinic acid derivatives ; Cytotoxicity ; Nitric oxide ; Biological activity ; Selectivity index
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：1 January, 2014
• 年：2014
• 卷：22
• 期：1
• 页码：585-593
• 全文大小：540 K

文摘

Here we report the synthesis and biological activity of new semi-synthetic derivatives of naturally occurring glycyrrhetinic acid bearing a 2-cyano-3-oxo-1-en moiety in the A-ring and double bonds and carbonyl groups in the C, D and E rings. Bioassays using murine macrophage-like and tumor cells show that compound 4, which differs from Soloxolone methyl by the absence of a 9(11)-double bond in the C-ring, displays anti-inflammatory and inhibitory activities with respect to tumor cells with a high selectivity index value.