the synthesis of glycyrrhetinic acid derivatives containing a nitrogen heterocycle and their antiproliferative effects in human leukemia cells甘草次酸衍生物合成的含氮杂环和抗增殖的影响在人类白血病细胞.pdfVIP

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the synthesis of glycyrrhetinic acid derivatives containing a nitrogen heterocycle and their antiproliferative effects in human leukemia cells甘草次酸衍生物合成的含氮杂环和抗增殖的影响在人类白血病细胞.pdf

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the synthesis of glycyrrhetinic acid derivatives containing a nitrogen heterocycle and their antiproliferative effects in human leukemia cells甘草次酸衍生物合成的含氮杂环和抗增殖的影响在人类白血病细胞

Molecules 2010, 15, 4439-4449; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article The Synthesis of Glycyrrhetinic Acid Derivatives Containing A Nitrogen Heterocycle and Their Antiproliferative Effects in Human Leukemia Cells 1 2 1 1 2 1 2 Yuan Gao , Xin Guo , Xiaojing Li , Dan Liu , Dandan Song , Ye Xu , Ming Sun , Yongkui Jing 3 and Linxiang Zhao 1,* 1 Key Laboratory of Structure-Based Drugs Design Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China 2 Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang 110016, China 3 Mount Sinai School of Medicine, One Gustave L. Levy Place, New York, NY 10029, USA * Author to whom correspondence should be addressed; E-Mail: zhaolinxiang@; Tel.: +86-24-2398-6420; Fax: +86-24-2389-6420. Received: 4 May 2010; in revised form: 11 June 2010 / Accepted: 17 June 2010 / Published: 21 June 2010 Abstract: Fifteen novel glycyrrhetinic acid derivatives containing a nitrogen heterocycle at C-30 and with different A-ring substituents were designed and synthesized. All of these derivatives have improved antiproliferative effects against human HL-60 leukemia cells. Compounds with a cyano-enone functionality on the A-ring exhibit greater growth inhibitory effects, compared to those with a 2-hydroxymethylene-3-keto, an isoxazole, or a 2-cyano-3-keto group. N-(2-cyano-3,11-diox