2017年12月15日
Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant
Bioorganic and Medicinal Chemistry
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- 巻
- 25
- 号
- 24
- 開始ページ
- 6563
- 終了ページ
- 6580
- 記述言語
- 英語
- 掲載種別
- 研究論文（学術雑誌）
- DOI
- 10.1016/j.bmc.2017.10.030
- 出版者・発行元
- Elsevier Ltd
A series of A-ring-modified lamellarin N analogues were designed, synthesized, and evaluated as potential noncovalent inhibitors of the EGFR T790M/L858R mutant, a causal factor in the drug-resistant non-small cell lung cancer. Several water-soluble ammonium- or guanidinium-tethered analogues exhibited good kinase inhibitory activities. The most promising analogue, 14f, displayed an excellent inhibitory profile against the T790M/L858R mutant [IC50 (WT) = 31.8 nM
IC50 (T790M/L858R) = 8.9 nM]. The effects of A-ring-substituents on activity were rationalized by docking studies.
IC50 (T790M/L858R) = 8.9 nM]. The effects of A-ring-substituents on activity were rationalized by docking studies.
- リンク情報
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- DOI
- https://doi.org/10.1016/j.bmc.2017.10.030
- PubMed
- https://www.ncbi.nlm.nih.gov/pubmed/29133033
- URL
- http://hdl.handle.net/10069/38936 本文へのリンクあり
- Scopus
- https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85033567176&origin=inward
- Scopus Citedby
- https://www.scopus.com/inward/citedby.uri?partnerID=HzOxMe3b&scp=85033567176&origin=inward
- ID情報
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- DOI : 10.1016/j.bmc.2017.10.030
- ISSN : 1464-3391
- ISSN : 0968-0896
- eISSN : 1464-3391
- ORCIDのPut Code : 38529013
- PubMed ID : 29133033
- SCOPUS ID : 85033567176