@article{oai:nagasaki-u.repo.nii.ac.jp:00001663,
 author = {Fukuda, Tsutomu and Umeki, Teppei and Tokushima, Keiji and Xiang, Gao and Yoshida, Yuki and Ishibashi, Fumito and Oku, Yusuke and Nishiya, Naoyuki and Uehara, Yoshimasa and Iwao, Masatomo},
 issue = {24},
 journal = {Bioorganic & Medicinal Chemistry},
 month = {Dec},
 note = {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., Bioorganic & Medicinal Chemistry, 25(24), pp.6563-6580; 2017},
 pages = {6563--6580},
 title = {Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant},
 volume = {25},
 year = {2017}
}