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j.bmc.2014.04.008.pdf | 336.03 kB | Adobe PDF | 見る/開く |
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dc.contributor.author | Takeuchi, Tomoki | en |
dc.contributor.author | Oishi, Shinya | en |
dc.contributor.author | Kaneda, Masato | en |
dc.contributor.author | Misu, Ryosuke | en |
dc.contributor.author | Ohno, Hiroaki | en |
dc.contributor.author | Sawada, Jun-ichi | en |
dc.contributor.author | Asai, Akira | en |
dc.contributor.author | Nakamura, Shinya | en |
dc.contributor.author | Nakanishi, Isao | en |
dc.contributor.author | Fujii, Nobutaka | en |
dc.contributor.alternative | 大石, 真也 | ja |
dc.date.accessioned | 2014-08-25T05:03:23Z | - |
dc.date.available | 2014-08-25T05:03:23Z | - |
dc.date.issued | 2014-06-15 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | http://hdl.handle.net/2433/189466 | - |
dc.description.abstract | Structure-activity relationship studies of diaryl amine-type KSP inhibitors were carried out. Diaryl amine derivatives with a pyridine ring or urea group were less active when compared with the parent carboline and carbazole derivatives. Optimization studies of a lactam-fused diphenylamine-type KSP inhibitor revealed that the aniline NH group and 3-CF3 phenyl group were indispensable for potent KSP inhibition. Modification with a seven-membered lactam-fused phenyl group and a 4-(trifluoromethyl)pyridin-2-yl group improved aqueous solubility while maintaining potent KSP inhibitory activity. From these studies, we identified novel diaryl amine-type KSP inhibitors with a favorable balance of potency and solubility. | en |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Elsevier BV | en |
dc.rights | © 2014 Elsevier Ltd. | en |
dc.rights | This is not the published version. Please cite only the published version. | en |
dc.rights | この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。 | ja |
dc.subject | Diaryl amine | en |
dc.subject | Kinesin spindle protein | en |
dc.subject | Aqueous solubility | en |
dc.title | Optimization of diaryl amine derivatives as kinesin spindle protein inhibitors. | en |
dc.type | journal article | - |
dc.type.niitype | Journal Article | - |
dc.identifier.ncid | AA10938083 | - |
dc.identifier.jtitle | Bioorganic & medicinal chemistry | en |
dc.identifier.volume | 22 | - |
dc.identifier.issue | 12 | - |
dc.identifier.spage | 3171 | - |
dc.identifier.epage | 3179 | - |
dc.relation.doi | 10.1016/j.bmc.2014.04.008 | - |
dc.textversion | author | - |
dc.identifier.pmid | 24794744 | - |
dcterms.accessRights | open access | - |
dc.identifier.pissn | 0968-0896 | - |
出現コレクション: | 学術雑誌掲載論文等 |
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