完整後設資料紀錄
DC 欄位 | 值 | 語言 |
---|---|---|
dc.contributor.author | Wu, Chia-Hsien | en_US |
dc.contributor.author | Coumar, Mohane Selvaraj | en_US |
dc.contributor.author | Chu, Chang-Ying | en_US |
dc.contributor.author | Lin, Wen-Hsing | en_US |
dc.contributor.author | Chen, Yi-Rong | en_US |
dc.contributor.author | Chen, Chiung-Tong | en_US |
dc.contributor.author | Shiao, Hui-Yi | en_US |
dc.contributor.author | Rafi, Shaik | en_US |
dc.contributor.author | Wang, Sing-Yi | en_US |
dc.contributor.author | Hsu, Hui | en_US |
dc.contributor.author | Chen, Chun-Hwa | en_US |
dc.contributor.author | Chang, Chun-Yu | en_US |
dc.contributor.author | Chang, Teng-Yuan | en_US |
dc.contributor.author | Lien, Tzu-Wen | en_US |
dc.contributor.author | Fang, Ming-Yu | en_US |
dc.contributor.author | Yeh, Kai-Chia | en_US |
dc.contributor.author | Chen, Ching-Ping | en_US |
dc.contributor.author | Yeh, Teng-Kuang | en_US |
dc.contributor.author | Hsieh, Su-Huei | en_US |
dc.contributor.author | Hsu, John T. -A. | en_US |
dc.contributor.author | Liao, Chun-Chen | en_US |
dc.contributor.author | Chao, Yu-Sheng | en_US |
dc.contributor.author | Hsieh, Hsing-Pang | en_US |
dc.date.accessioned | 2019-04-02T06:00:18Z | - |
dc.date.available | 2019-04-02T06:00:18Z | - |
dc.date.issued | 2010-10-28 | en_US |
dc.identifier.issn | 0022-2623 | en_US |
dc.identifier.uri | http://dx.doi.org/10.1021/jm100607r | en_US |
dc.identifier.uri | http://hdl.handle.net/11536/150090 | - |
dc.description.abstract | HTS hit 7 was modified through hybrid design strategy to introduce a chiral side chain followed by introduction of Michael acceptor group to obtain potent EGFR kinase inhibitors 11 and 19. Both 11 and 19 showed over 3 orders of magnitude enhanced HCC827 antiproliferative activity compared to HTS hit 7 and also inhibited gefitinib-resistant double mutant (DM, T790M/L858R) EGFR kinase at nanomolar concentration. Moreover, treatment with 19 shrinked tumor in nude mice xenograft model. | en_US |
dc.language.iso | en_US | en_US |
dc.title | Design and Synthesis of Tetrahydropyridothieno[2,3-d]pyrimidine Scaffold Based Epidermal Growth Factor Receptor (EGFR) Kinase Inhibitors: The Role of Side Chain Chirality and Michael Acceptor Group for Maximal Potency | en_US |
dc.type | Article | en_US |
dc.identifier.doi | 10.1021/jm100607r | en_US |
dc.identifier.journal | JOURNAL OF MEDICINAL CHEMISTRY | en_US |
dc.citation.volume | 53 | en_US |
dc.citation.spage | 7316 | en_US |
dc.citation.epage | 7326 | en_US |
dc.contributor.department | 生物科技學系 | zh_TW |
dc.contributor.department | Department of Biological Science and Technology | en_US |
dc.identifier.wosnumber | WOS:000283106300005 | en_US |
dc.citation.woscount | 66 | en_US |
顯示於類別: | 期刊論文 |