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Structural optimization of 10-methyl-aplog-1, a simplified analog of debromoaplysiatoxin, as an anticancer lead
https://oacis.repo.nii.ac.jp/records/1738
https://oacis.repo.nii.ac.jp/records/1738268e0c2e-0eda-4b76-87d3-8a3ef7210bca
Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2019-05-27 | |||||
タイトル | ||||||
タイトル | Structural optimization of 10-methyl-aplog-1, a simplified analog of debromoaplysiatoxin, as an anticancer lead | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
主題 | anti-proliferative, cancer, debromoaplysiatoxin, protein kinase C, tumor promoter | |||||
資源タイプ | ||||||
資源タイプ | journal article | |||||
アクセス権 | ||||||
アクセス権 | metadata only access | |||||
著者 |
Kikumori, Masayuki
× Kikumori, Masayuki× Yanagita, Ryo C.× Tokuda, Harukuni× Suenaga, Kiyotake× Nagai, Hiroshi× Irie, Kazuhiro |
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書誌情報 |
Bioscience, Biotechnology, and Biochemistry 巻 80, 号 2, p. 221-231, 発行日 2016 |
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抄録 | ||||||
内容記述 | Aplog-1 is a simplified analog of debromoaplysiatoxin (DAT) with potent tumor-promoting and proinflammatory activities. Aplog-1 and DAT exhibited anti-proliferative activities against several human cancer cell lines, whereas aplog-1 did not have tumor-promoting nor proinflammatory activities. We have recently found 10-methyl-aplog-1 (1) to have strong anti-proliferative activity compared with aplog-1. To further investigate the structural factors involved in the tumor-promoting, proinflammatory, and anti-proliferative activities, two dimethyl derivatives of aplog-1 (2, 3) were synthesized, where two methyl groups were installed at positions 4 and 10 or 10 and 12. 10,12-Dimethyl-aplog-1 (2) had stronger inhibitory effects on the growth of several human cancer cell lines than 1 and DAT, but exhibited no tumor-promoting and proinflammatory activities. In contrast, 4,10-dimethyl-aplog-1 (3) displayed weak tumor-promoting and proinflammatory activities along with anti-proliferative activity similar to that of 1 and DAT. Compound 2 would be the optimized seed for anticancer drugs among the simplified analogs of DAT. | |||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 09168451 | |||||
書誌レコードID | ||||||
収録物識別子タイプ | NCID | |||||
収録物識別子 | AA10824164 | |||||
DOI | ||||||
識別子タイプ | DOI | |||||
関連識別子 | https://doi.org/10.1080/09168451.2015.1091718 | |||||
情報源 | ||||||
関連識別子 | https://doi.org/10.1080/09168451.2015.1091718 | |||||
関連名称 | Publisher's Version/PDF (OpenAccess) | |||||
情報源 | ||||||
関連識別子 | http://www.jsbba.or.jp/ | |||||
関連名称 | 日本農芸化学会 | |||||
情報源 | ||||||
関連識別子 | https://kaken.nii.ac.jp/ja/grant/KAKENHI-PROJECT-16K01911/ | |||||
関連名称 | KAKEN研究課題: 海洋危険生物の有する痛み惹起物質の解明 | |||||
情報源 | ||||||
関連識別子 | https://nrid.nii.ac.jp/ja/nrid/1000050291026/ | |||||
関連名称 | 研究代表者: 永井 宏史 (東京海洋大学) | |||||
件名 | ||||||
主題 | 科学研究費研究成果 | |||||
出版者 | ||||||
出版者 | 日本農芸化学会 | |||||
科学研究費研究課題 | ||||||
主題 | 海洋危険生物の有する痛み惹起物質の解明 | |||||
研究課題番号 | ||||||
内容記述 | 16K01911 |