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丁晔, 张珍珍, 黄张建, 牟伊, 季晖, 赖宜生, 张奕华. 新型齐墩果酸衍生物的合成及抗肿瘤活性[J]. 中国药科大学学报, 2011, 42(5): 385-391.
引用本文: 丁晔, 张珍珍, 黄张建, 牟伊, 季晖, 赖宜生, 张奕华. 新型齐墩果酸衍生物的合成及抗肿瘤活性[J]. 中国药科大学学报, 2011, 42(5): 385-391.
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DING Ye, ZHANG Zhen-zhen, HUANG Zhang-jian, MOU Yi, JI Hui, LAI Yi-sheng, ZHANG Yi-hua. Synthesis and anticancer activity of novel oleanolic acid derivatives[J]. Journal of China Pharmaceutical University, 2011, 42(5): 385-391.
Citation: DING Ye, ZHANG Zhen-zhen, HUANG Zhang-jian, MOU Yi, JI Hui, LAI Yi-sheng, ZHANG Yi-hua. Synthesis and anticancer activity of novel oleanolic acid derivatives[J]. Journal of China Pharmaceutical University, 2011, 42(5): 385-391.
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新型齐墩果酸衍生物的合成及抗肿瘤活性

Synthesis and anticancer activity of novel oleanolic acid derivatives

    摘要
  • 摘要: 以齐墩果酸（OA）为先导化合物，经C28位羧基保护、C3位乙酰化、C12位氧化、C11位溴代后消除等7步连续反应合成了具有α,β-不饱和酮结构的OA衍生物；再以甘氨酸为连接基团，将不同取代的呋咱氮氧化物类一氧化氮供体与其偶联，获得新型OA衍生物，其结构经IR、MS及1H NMR确证。采用MTT法测定目标物和部分中间体对4种人肿瘤细胞的增殖抑制活性。结果表明，所有目标物的抗肿瘤活性均显著优于OA，其中 10a-10e 和 10i 对人肝癌HepG2细胞的增殖抑制活性与阳性对照药2-氰基-3，12-二氧代齐墩果烷-1，9（11）-二烯-28-羧酸甲酯（CDDO-Me）相当。

     

    Abstract: Starting from oleanolic acid (OA),the target compounds ( 10a-10i ) were synthesized via introductingα,β-unsaturated ketone moiety to OA by 7-step successive reactions including benzylation,acetylation,oxidization,bromine substitution-elimination,etc.,followed by coupling of C28-carboxyl with substituted furoxans via a glycine linker.All the target compounds were identified by IR,MS and 1H NMR.MTT assay results showed that compounds 10a-10i displayed much stronger inhibitory effects than OA on the proliferation of four human tumor cell lines.The anti-proliferative activity of 10a-10e and 10i against human hepatoma HepG2 cell was comparable to that of the positive control 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid methyl ester (CDDO-Me).

     

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