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Synthesis, cytotoxic activities and cell cycle arrest profiles of naphtho[2,1-alpha]pyrrolo[3,4-c]carbazole-5,7(6H, 12H)-dione glycosides

文献类型：期刊论文

作者Ding, Ning1,2; Du, Xiaoguang3; Zhang, Wei1; Lu, Zhichao4; Li, Yingxia1
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2011-06-15
卷号21期号:12页码:3531-3535
关键词Indolocarbazole Cytotoxic Rebeccamycin Cell-cycle Glycoside
ISSN号0960-894X
DOI10.1016/j.bmcl.2011.04.145
文献子类Article
英文摘要Naphtho[2,1-alpha] pyrrolo[3,4-c]carbazole-5,7(6H, 12H)-dione (NPCD) is known to be a very potent and selective cyclin D1-CDK4 inhibitors and could induce strong G1 phase arrest in breast tumor cell lines. In this work, the synthesis of five NPCD glycosides and their cytotoxic activities against eight tumor cell lines are presented, as well as the investigation of their cell cycle arrest profiles. The results showed that the introduction of a sugar moiety onto NPCD did not affect much of their cytotoxic activities, while the subtle structure of the sugar moiety affected the underlying mechanism strongly. In addition, NPCD showed distinct cell-cycle arrest profiles in BxPC3 prostate cells and MCF-7 breast cells, while NPCD glycosides shared similar cell cycle arrest profiles in MCF-7 and BxPC3 cells, which also indicated that not only the indolocarbazole framework as well known before but the sugar moiety can have a profound impact on the mechanism of action for these types of compounds. (C) 2011 Elsevier Ltd. All rights reserved.
WOS关键词BIOLOGICAL EVALUATION ; CDK INHIBITORS ; REBECCAMYCIN ; ANTITUMOR ; ANALOGS ; CARBAZOLES ; D1-CDK4 ; AGENTS
资助项目National High-tech R&D Program of China[2011AA09070105] ; State Key Laboratory of Drug Research[SIMM0812KF-08]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000291145900006
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/278500]  
专题新药研究国家重点实验室
中科院受体结构与功能重点实验室
通讯作者Li, Yingxia
作者单位1.Fudan Univ, Dept Med Chem, Sch Pharm, Shanghai 201203, Peoples R China;
2.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
3.Chinese Acad Sci, Div Antitumor Pharmacol, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
4.Ocean Univ China, Sch Med & Pharm, Qingdao 266003, Peoples R China
推荐引用方式
GB/T 7714		 Ding, Ning,Du, Xiaoguang,Zhang, Wei,et al. Synthesis, cytotoxic activities and cell cycle arrest profiles of naphtho[2,1-alpha]pyrrolo[3,4-c]carbazole-5,7(6H, 12H)-dione glycosides[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2011,21(12):3531-3535.
APA Ding, Ning,Du, Xiaoguang,Zhang, Wei,Lu, Zhichao,&Li, Yingxia.(2011).Synthesis, cytotoxic activities and cell cycle arrest profiles of naphtho[2,1-alpha]pyrrolo[3,4-c]carbazole-5,7(6H, 12H)-dione glycosides.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,21(12),3531-3535.
MLA Ding, Ning,et al."Synthesis, cytotoxic activities and cell cycle arrest profiles of naphtho[2,1-alpha]pyrrolo[3,4-c]carbazole-5,7(6H, 12H)-dione glycosides".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 21.12(2011):3531-3535.

入库方式： OAI收割

来源：上海药物研究所

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