Design, synthesis and biological evaluation of C(6)-indole celastrol derivatives as potential antitumor agents

Tang Kaiyong; Huang Jinwen; Pan Junfang; Zhang Xuan; Lu Wei

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Design, synthesis and biological evaluation of C(6)-indole celastrol derivatives as potential antitumor agents

机译：C（6） - 吲哚Celastrol衍生物作为潜在抗肿瘤剂的设计，合成和生物学评价

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Celastrol is a natural triterpenoid which possesses diverse pharmacological activities including potent antitumor activity. Previously, we reported a C(6)-modified celastrol derivative NST001A which possesses cytotoxic activity against Colon 205 cells with a 60 nM IC50 value. To further explore the structure activity relationships, a new class of C(6)-indole substituted celastrol derivatives were designed and synthesized. Biological evaluation of these compounds includes their cytotoxic activity against human hepatocellular carcinoma Bel7402 and human glioblastoma cell line H4. Among all these semisynthetic analogues, compound 4f and 4h displayed excellent in vitro antiproliferative activities against Bel7402 cancer cells (IC50 = 0.02 mu M and 0.01 mu M, respectively).

机译：Celastrol是一种自然的三萜，具有不同的药理学活动，包括有效的抗肿瘤活性。以前，我们报道了C（6）制定的Celastrol衍生物NST001A，其具有针对具有60nM IC50值的冒号205个细胞的细胞毒性活性。为了进一步探索结构活动关系，设计并合成了一类新的C类C（6）-DOMEL取代的Celastrol衍生物。这些化合物的生物学评价包括对人肝细胞癌BEL7402和人胶质母细胞瘤细胞系H4的细胞毒性活性。在所有这些半合成类似物中，化合物4F和4H在Bel7402癌细胞上显示出优异的体外抗增殖活动（IC50 =0.02μm和0.01μm）。

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《RSC Advances》 |2015年第25期|共4页
作者
Tang Kaiyong; Huang Jinwen; Pan Junfang; Zhang Xuan; Lu Wei;
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作者单位

E China Normal Univ Shanghai Engn Res Ctr Mol Therapeut &

New Drug De Inst Drug Discovery &

Dev Shanghai 200062 Peoples R China;

Shanghai Hotmed Sci Co Ltd Shanghai 201201 Peoples R China;

Shanghai Hotmed Sci Co Ltd Shanghai 201201 Peoples R China;

E China Normal Univ Shanghai Engn Res Ctr Mol Therapeut &

New Drug De Inst Drug Discovery &

Dev Shanghai 200062 Peoples R China;

E China Normal Univ Shanghai Engn Res Ctr Mol Therapeut &

New Drug De Inst Drug Discovery &

Dev Shanghai 200062 Peoples R China;

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正文语种 eng
中图分类化学;
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1. Design, synthesis and biological evaluation of C(6)-indole celastrol derivatives as potential antitumor agents [J] . Tang Kaiyong, Huang Jinwen, Pan Junfang, RSC Advances . 2015,第25期

机译：C（6） - 吲哚Celastrol衍生物作为潜在抗肿瘤剂的设计，合成和生物学评价
2. Design, Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents [J] . Guangming Wu, Jafeng Zeng, Jinwen Huang, Molecules . 2014,第7期

机译：C（6）修饰的Celastrol衍生物作为潜在抗肿瘤药物的设计，合成和生物学评估
3. Design, synthesis, biological evaluation and structure-activity relationship of sophoridine derivatives bearing pyrrole or indole scaffold as potential antitumor agents [J] . Li Zheng, Luo Mengyang, Cai Bin, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2018,第期

机译：携带吡咯或吲哚支架作为潜在抗肿瘤剂的Sophoridine衍生物的设计，合成，生物学评价和结构 - 活性关系
4. Design, Synthesis and Biological Evaluation of the Novel Antitumor Agent 2H-benzob1, 4oxazin-3(4H)-one and Its Derivatives [C] . Huanhuan Li, Kailin Han, Qiannan Guo, International symposium on IT in medicine and education . 2014

机译：新型抗肿瘤药2H-苯并b 1,4恶嗪-3（4H）-one及其衍生物的设计，合成及生物学评价
5. The design, synthesis, and biological evaluation of novel antitumor agents. [D] . Mathews, Jude Elizabeth. 1996

机译：新型抗肿瘤药的设计，合成和生物学评估。
6. Design Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents [O] . Kaiyong Tang, Qingqing Huang, Jafeng Zeng, 2014

机译：C（6）修饰的Celastrol衍生物作为潜在抗肿瘤药物的设计合成和生物学评估
7. Design, Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents [O] . Kaiyong Tang, Qingqing Huang, Jafeng Zeng, 2014

机译：C（6） - 改性Celastrol衍生物作为潜在抗肿瘤药物的设计，合成及生物学评价

Design, synthesis and biological evaluation of C(6)-indole celastrol derivatives as potential antitumor agents

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