Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.

• 入江, 一浩

• Kamachi, Hiroaki

• Tanaka, Keisuke

• Murakami, Akira

• Nakagawa, Yu

• Tokuda, Harukuni

• Nagai, Hiroshi

• Irie, Kazuhiro

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.

収録刊行物

• Bioorganic & medicinal chemistry letters

  Bioorganic & medicinal chemistry letters 20 (20), 6064-6066, 2010-10-15

  Elsevier Ltd

キーワード

• Protein kinase C
• Tumor promoter
• Bryostatin
• Antiproliferative
• Epstein-Barr virus
• Aplysiatoxin
• Phorbol ester

詳細情報

• CRID: 1050001201940332288
• NII論文ID: 120002561292
• NII書誌ID: AA1079577X
• ISSN: 0960894X
• HANDLE: 2433/130698
• 本文言語コード: en
• 資料種別: journal article
• データソース種別:
  • IRDB
  • CiNii Articles