Design, Synthesis, and Evaluation of Ribose-Modified Anilinopyrimidine Derivatives as EGFR Tyrosine Kinase Inhibitors
文献类型：期刊论文
| 作者 | Hu, Xiuqin1; Wang, Disha1; Tong, Yi1; Tong, Linjiang2; Wang, Xia1; Zhu, Lili1; Xie, Hua2 ; Li, Shiliang1; Yang, You1; Xu, Yufang1
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| 刊名 | FRONTIERS IN CHEMISTRY
 |
| 出版日期 | 2017-11-15 |
| 卷号 | 5 |
| 关键词 | EGFR tyrosine kinase inhibitors anilinopyrtmidine glycosides carbohydrate-based drugs |
| ISSN号 | 2296-2646 |
| DOI | 10.3389/fchem.2017.00101 |
| 文献子类 | Article |
| 英文摘要 | The synthesis of a series of ribose-modified anilinopyrimidine derivatives was efficiently achieved by utilizing DBU or tBuOLi-promoted coupling of ribosyl alcohols with 2,4,5-trichloropyrimidine as key step. Preliminary biological evaluation of this type of compounds as new EGFR tyrosine kinase inhibitors for combating EGFR L858R/T790M mutant associated with drug resistance in the treatment of non-small cell lung cancer revealed that 3-N-acryloyl-5-O-anilinopyrimidine ribose derivative la possessed potent and specific inhibitory activity against EGER L858R/1790M over WT EGER. Based upon molecular docking studies of the binding mode between compound la and EGFR, the distance between the Michael receptor and the pyrimidine scaffold is considered as an important factor for the inhibitory potency and future design of selective EGFR tyrosine kinase inhibitors against EGFR L858R/T790M mutants. |
| WOS关键词 | GROWTH-FACTOR RECEPTOR ; CELL LUNG-CANCER ; ACQUIRED-RESISTANCE ; MUTANT ; AZD9291 ; T790M ; DISCOVERY ; POTENT ; STRATEGIES ; MUTATIONS |
| 资助项目 | National Thousand Young Talents Program[YC0130518] ; National Thousand Young Talents Program[YC0140103] ; Shanghai Committee of Science and Technology[14431902100] ; Shanghai Pujiang Program[15PJ1401500] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000415164500001 |
| 出版者 | FRONTIERS MEDIA SA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272401]  |
| 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 |
| 通讯作者 | Yang, You; Xu, Yufang |
| 作者单位 | 1.East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Hu, Xiuqin,Wang, Disha,Tong, Yi,et al. Design, Synthesis, and Evaluation of Ribose-Modified Anilinopyrimidine Derivatives as EGFR Tyrosine Kinase Inhibitors[J]. FRONTIERS IN CHEMISTRY,2017,5. |
| APA | Hu, Xiuqin.,Wang, Disha.,Tong, Yi.,Tong, Linjiang.,Wang, Xia.,...&Xu, Yufang.(2017).Design, Synthesis, and Evaluation of Ribose-Modified Anilinopyrimidine Derivatives as EGFR Tyrosine Kinase Inhibitors.FRONTIERS IN CHEMISTRY,5. |
| MLA | Hu, Xiuqin,et al."Design, Synthesis, and Evaluation of Ribose-Modified Anilinopyrimidine Derivatives as EGFR Tyrosine Kinase Inhibitors".FRONTIERS IN CHEMISTRY 5(2017). |
入库方式： OAI收割
来源：上海药物研究所
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