discoveringnovel3nitroquinolinesasanewclassofanticanceragents
文献类型：期刊论文
| 作者 | Haihong LI; He HUANG; Xiuhua ZHANG; Xiaomin LUO ; Liping LIN; Hualiang JIANG; Jian DING; Kaixian CHEN; Hong LIU
|
| 刊名 | actapharmacologicasinica
 |
| 出版日期 | 2008 |
| 卷号 | 29期号:12页码:1529 |
| 关键词 | GROWTH-FACTOR RECEPTOR TYROSINE KINASE INHIBITORS SITE INHIBITORS EGF-R PROTEIN ANALOGS DESIGN CANCER 3-nitroquinoline epidermal growth factor receptor tyrosine kinase inhibitor molecular modeling |
| ISSN号 | 1671-4083 |
| DOI | 10.1111/j.1745-7254.2008.00907.x |
| 英文摘要 | Aim: To design and synthesize a novel class of antitumor agents, featuring the 3-nitroquinoline framework. Methods: Based on the enzyme-binding features of Ekb1, introducing a nitro group at the 3-position of the quinoline core, a series of novel 3-nitroquinolines was designed and synthesized. The inhibition of epidermal growth factor receptor (EGFR) activity by these compounds was evaluated and analyzed by the sulforhodamine B assay for their inhibitory activities toward human epidermoid carcinoma (A431) cells and breast cancer (MDA-MB-468) cells, which are known to overexpress the EGFR kinase. Results: A series of novel 3-nitroquinoline derivatives were synthesized and evaluated for their antiproliferative effect against the EGFR-overexpressing tumor cell lines. Several compounds for concentration-response studies showed prominent inhibitory activities with IC50 values in the micromolar or nanomolar range. The structure-activity relationship was discussed in terms of the inhibitory activity against the proliferation of 2 human carcinoma cell lines. Conclusion: This study was the first to identify new structural types of antiproliferative agents against the EGFR-overexpressing tumor cell lines by the incorporation of the nitro group at the 3-position of the quinoline core structure, providing promising new templates for the further development of anticancer agents. |
| 资助项目 | [State Key Program of Basic Research of China] ; [National Natural Science Foundation of China] ; [863 Hi-Tech Program of China] |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/285668]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Haihong LI,He HUANG,Xiuhua ZHANG,et al. discoveringnovel3nitroquinolinesasanewclassofanticanceragents[J]. actapharmacologicasinica,2008,29(12):1529. |
| APA | Haihong LI.,He HUANG.,Xiuhua ZHANG.,Xiaomin LUO.,Liping LIN.,...&Hong LIU.(2008).discoveringnovel3nitroquinolinesasanewclassofanticanceragents.actapharmacologicasinica,29(12),1529. |
| MLA | Haihong LI,et al."discoveringnovel3nitroquinolinesasanewclassofanticanceragents".actapharmacologicasinica 29.12(2008):1529. |
入库方式： OAI收割
来源：上海药物研究所
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