Interaction of bisbenzimidazole-substituted carbazole derivatives with G-quadruplexes and living cells
文献类型：期刊论文
| 作者 | Wei, Yongbiao1,2; Zhang, Xin1; Wang, Linlin1; Liu, Ying1; Bing, Tao1; Liu, Xiangjun1; Shangguan, Dihua1 |
| 刊名 | RSC ADVANCES
 |
| 出版日期 | 2015 |
| 卷号 | 5期号:93页码:75911-75917 |
| 英文摘要 | G-quadruplex (G4) ligands have potential as chemotherapeutic agents because of the important roles of G4s in regulation of genomic function. Previously, we have developed a fluorescent probe (termed as BPBC) with excellent selectivity to parallel G4s, which possesses a V-shaped bisbenzimidazole-substituted carbazole planar core and two methylpiperazine side arms. Here, we further investigated the interactions of BPBC derivatives with different DNA and living cells. The spectral analysis showed that non-substituted bisbenzimidazole-substituted carbazole (7c) and bisdimethylamino-substituted 7c (7b) exhibited good selectivity to parallel G4s. The binding affinities of BPBC derivatives to parallel G4s were BPBC > 7b >= 7c. BPBC and 7b entered living cells and mainly located in the cytoplasma and nucleoli; 7c mainly located in the lysosome. BPBC exhibited the highest cytotoxicity with IC50 around 1 mu M. Our results suggest that the bisbenzimidazole-substituted carbazole core is the key factor for selectively binding BPBC derivatives to parallel G4s; the side arms can change their affinity to specific G4s, as well as their interaction with cells. Further optimization of the side arms will provide the opportunity to obtain chemotherapeutic agents targeting specific G4s in cells. |
| 收录类别 | SCI |
| 语种 | 英语 |
| 公开日期 | 2016-05-09 |
| 源URL | [http://ir.iccas.ac.cn/handle/121111/28373]  |
| 专题 | 化学研究所_活体分析化学实验室 |
| 作者单位 | 1.Chinese Acad Sci, Inst Chem, Beijing Natl Lab Mol Sci, Key Lab Analyt Chem Living Biosyst, Beijing 100190, Peoples R China 2.Guangxi Med Univ, Sch Pharmaceut Sci, Dept Pharmaceut Chem, Nanning 530021, Guangxi, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wei, Yongbiao,Zhang, Xin,Wang, Linlin,et al. Interaction of bisbenzimidazole-substituted carbazole derivatives with G-quadruplexes and living cells[J]. RSC ADVANCES,2015,5(93):75911-75917. |
| APA | Wei, Yongbiao.,Zhang, Xin.,Wang, Linlin.,Liu, Ying.,Bing, Tao.,...&Shangguan, Dihua.(2015).Interaction of bisbenzimidazole-substituted carbazole derivatives with G-quadruplexes and living cells.RSC ADVANCES,5(93),75911-75917. |
| MLA | Wei, Yongbiao,et al."Interaction of bisbenzimidazole-substituted carbazole derivatives with G-quadruplexes and living cells".RSC ADVANCES 5.93(2015):75911-75917. |
入库方式： OAI收割
来源：化学研究所
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