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ファイル | 記述 | サイズ | フォーマット | |
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j.bmc.2014.04.008.pdf | 336.03 kB | Adobe PDF | 見る/開く |
タイトル: | Optimization of diaryl amine derivatives as kinesin spindle protein inhibitors. |
著者: | Takeuchi, Tomoki Oishi, Shinya https://orcid.org/0000-0002-2833-2539 (unconfirmed) Kaneda, Masato Misu, Ryosuke Ohno, Hiroaki https://orcid.org/0000-0002-3246-4809 (unconfirmed) Sawada, Jun-ichi Asai, Akira Nakamura, Shinya Nakanishi, Isao Fujii, Nobutaka |
著者名の別形: | 大石, 真也 |
キーワード: | Diaryl amine Kinesin spindle protein Aqueous solubility |
発行日: | 15-Jun-2014 |
出版者: | Elsevier BV |
誌名: | Bioorganic & medicinal chemistry |
巻: | 22 |
号: | 12 |
開始ページ: | 3171 |
終了ページ: | 3179 |
抄録: | 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. |
著作権等: | © 2014 Elsevier Ltd. This is not the published version. Please cite only the published version. 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。 |
URI: | http://hdl.handle.net/2433/189466 |
DOI(出版社版): | 10.1016/j.bmc.2014.04.008 |
PubMed ID: | 24794744 |
出現コレクション: | 学術雑誌掲載論文等 |
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