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j.bmcl.2010.08.051.pdf | 460.82 kB | Adobe PDF | 見る/開く |
タイトル: | Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity. |
著者: | Yanagita, Ryo C Kamachi, Hiroaki Tanaka, Keisuke Murakami, Akira Nakagawa, Yu Tokuda, Harukuni Nagai, Hiroshi Irie, Kazuhiro https://orcid.org/0000-0001-7109-8568 (unconfirmed) |
著者名の別形: | 入江, 一浩 |
キーワード: | Protein kinase C Tumor promoter Bryostatin Antiproliferative Epstein-Barr virus Aplysiatoxin Phorbol ester |
発行日: | 15-Oct-2010 |
出版者: | Elsevier Ltd |
誌名: | Bioorganic & medicinal chemistry letters |
巻: | 20 |
号: | 20 |
開始ページ: | 6064 |
終了ページ: | 6066 |
抄録: | The 18-deoxy derivative (3) of a simplified analogue (1) of aplysiatoxin with antiproliferative activity was synthesized to examine the role of the phenolic hydroxyl group at position 18 in the biological activities of 1. Compound 3 as well as 1 showed significant affinity for protein kinase Cδ (PKCδ), and the antiproliferative activity of 3 was slightly higher than that of 1. However, the anti-tumor-promoting activity of 3 was less than that of 1 in vitro, suggesting that the phenolic hydroxyl group of 1 is necessary for the anti-tumor-promoting activity but not for the binding of PKCδ and antiproliferative activity. Moreover, PKC isozyme selectivity of 3 was similar to that of 1, suggesting non-PKC receptors for these compounds to play some roles in the anti-tumor-promoting activity of 1. |
著作権等: | © 2010 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/2433/130698 |
DOI(出版社版): | 10.1016/j.bmcl.2010.08.051 |
PubMed ID: | 20817520 |
出現コレクション: | 学術雑誌掲載論文等 |
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