Nitric oxide donating anilinopyrimidines: Synthesis and biological evaluation as EGFR inhibitors
文献类型：期刊论文
| 作者 | Han, C; Huang, ZJ; Zheng, C; Wan, LD; Lai, YS; Peng, SX; Ding, K; Ji, HB; Zhang, YH |
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2013 |
| 卷号 | 66期号:1页码:82-90 |
| 关键词 | Nitric oxide EGFR inhibitor Anilinopyrimidine Antiproliferative activity WZ4002 |
| 通讯作者 | Zhang, YH (reprint author), China Pharmaceut Univ, Ctr Drug Discovery, Nanjing 210009, Jiangsu, Peoples R China.,ding_ke@gibh.ac.cn ; hbji@sibs.accn ; zyhtgd@163.com |
| 英文摘要 | To search for potent nitric oxide (NO) donating epidermal growth factor receptor (EGFR) inhibitors, a series of phenylsulfonylfuroxan-based anilinopyrimidines 10a-h were synthesized and biologically evaluated. Compounds 10f-h exhibited potent inhibitory activity against EGFR L858R/T790M and were as potent as WZ4002 in inhibition of H1975 cells harboring EGFR L858R/T790M. Additionally, 10h produced high levels of NO in H1975 cells but not in normal human cells, and its antiproliferative activity was diminished by hemoglobin, an NO scavenger. Furthermore, 10h inhibited EGFR activation and downstream signaling in H1975 cells. These results suggest that the strong antiproliferative activity of 10h could be attributed to the synergic effects of high levels of NO production and inhibition of EGFR and downstream signaling in the cancer cells. (C) 2013 Elsevier Masson SAS. All rights reserved. |
| 学科主题 | Pharmacology & Pharmacy |
| 类目[WOS] | Chemistry, Medicinal |
| 关键词[WOS] | GROWTH-FACTOR RECEPTOR ; CELL LUNG-CANCER ; ANTIHEPATOCELLULAR CARCINOMA ACTIVITY ; TYROSINE KINASE INHIBITOR ; PAN-ERBB INHIBITOR ; PHASE-II TRIAL ; DRUG-RESISTANCE ; DERIVATIVES ; GEFITINIB ; FUROXANS |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000323628500008 |
| 版本 | 出版稿 |
| 源URL | [http://202.127.25.143/handle/331003/510]  |
| 专题 | 上海生化细胞研究所_上海生科院生化细胞研究所 |
| 推荐引用方式 GB/T 7714 | Han, C,Huang, ZJ,Zheng, C,et al. Nitric oxide donating anilinopyrimidines: Synthesis and biological evaluation as EGFR inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2013,66(1):82-90. |
| APA | Han, C.,Huang, ZJ.,Zheng, C.,Wan, LD.,Lai, YS.,...&Zhang, YH.(2013).Nitric oxide donating anilinopyrimidines: Synthesis and biological evaluation as EGFR inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,66(1),82-90. |
| MLA | Han, C,et al."Nitric oxide donating anilinopyrimidines: Synthesis and biological evaluation as EGFR inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 66.1(2013):82-90. |
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