Design and synthesis of pyrido[3,2-a]carbazole derivatives and their analogues as potent antitumour agents
文献类型：期刊论文
| 作者 | Li, Bo1,2; Yue, Zhi-Zhou1; Feng, Jian-Ming2; He, Qian2 ; Miao, Ze-Hong2; Yang, Chun-Hao2
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2013-08 |
| 卷号 | 66页码:531-539 |
| 关键词 | Pyrido[3,2-alpha]carbazole Analogues Synthetic approach Antitumour profile Potency |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2013.05.045 |
| 文献子类 | Article |
| 英文摘要 | A series of pyrido[3,2-a]carbazole derivatives and their analogues have been prepared and evaluated for their antitumour activity against human lung cancer A549 cells and colon cancer HT29 cells. The intermediates 4a-4k are successfully synthesized from 1a-1k and ethyl 2-(3-bromopyridin-2-yl)acetate by Knoevenagel condensation and intramolecular Heck-type reaction, and this is a novel and efficient synthetic approach to the core scaffold of the target compounds. These target compounds have shown an interesting antitumour profile towards the tested cell lines with IC50 values ranging from 0.07 mu M to 4.45 mu M. Among all the compounds synthesized, 8 compounds show higher potency than R16, 12 compounds are as potent as R16, and 6 compounds are less potent than R16. The best compound 24 is 7 times and approximately 10 times as potent as R16 against A549 and HT29 cells, respectively. (c) 2013 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | LEUKEMIA GROUP-B ; AMONAFIDE ; NAPHTHALIMIDES ; ARYLATION ; CANCER ; DNA |
| 资助项目 | Ministry of Science and Technology of China (Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program")[2012ZX09301001-001] ; Ministry of Science and Technology of China (Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program")[2012ZX09301-001-002] ; National Natural Science Foundation of China[81025020] ; Chinese Academy of Sciences ("Interdisciplinary Cooperation Team" Program for Science and Technology Innovation)[00000000] ; SKLDR/SIMM[SIMM1203ZZ-0103] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000323628500055 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277514]  |
| 专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物发现与设计中心 药物化学研究室 |
| 通讯作者 | Miao, Ze-Hong |
| 作者单位 | 1.Wuhan Univ Technol, Dept Pharmaceut Engn, Sch Chem Engn, Wuhan 430070, Hubei, Peoples R China; 2.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Bo,Yue, Zhi-Zhou,Feng, Jian-Ming,et al. Design and synthesis of pyrido[3,2-a]carbazole derivatives and their analogues as potent antitumour agents[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2013,66:531-539. |
| APA | Li, Bo,Yue, Zhi-Zhou,Feng, Jian-Ming,He, Qian,Miao, Ze-Hong,&Yang, Chun-Hao.(2013).Design and synthesis of pyrido[3,2-a]carbazole derivatives and their analogues as potent antitumour agents.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,66,531-539. |
| MLA | Li, Bo,et al."Design and synthesis of pyrido[3,2-a]carbazole derivatives and their analogues as potent antitumour agents".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 66(2013):531-539. |
入库方式： OAI收割
来源：上海药物研究所
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