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Title: Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.
Authors: Yanagita, Ryo C
Kamachi, Hiroaki
Tanaka, Keisuke
Murakami, Akira  KAKEN_id
Nakagawa, Yu
Tokuda, Harukuni
Nagai, Hiroshi
Irie, Kazuhiro  kyouindb  KAKEN_id  orcid https://orcid.org/0000-0001-7109-8568 (unconfirmed)
Author's alias: 入江, 一浩
Keywords: Protein kinase C
Tumor promoter
Bryostatin
Antiproliferative
Epstein-Barr virus
Aplysiatoxin
Phorbol ester
Issue Date: 15-Oct-2010
Publisher: Elsevier Ltd
Journal title: Bioorganic & medicinal chemistry letters
Volume: 20
Issue: 20
Start page: 6064
End page: 6066
Abstract: 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.
Rights: © 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(Published Version): 10.1016/j.bmcl.2010.08.051
PubMed ID: 20817520
Appears in Collections:Journal Articles

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