Optically active iodohelicene derivatives exhibit histamine N-methyl transferase inhibitory activity

Wataru Ichinose, Tsukasa Sawato, Haruna Kitano, Yasuhiro Shinozaki, Mieko Arisawa, Nozomi Saito, Takeo Yoshikawa, Masahiko Yamaguchi

研究成果: ジャーナルへの寄稿学術誌査読

1 被引用数 (Scopus)

抄録

Optically active helicene derivatives inhibit the activity on histamine N-methyl transferase (HNMT). Specifically, methyl (P)-1,12-dimethylbenzo[c]phenanthrene-8-carboxylate with 6-iodo and 5-trifluoromethanesulfonyloxy groups inhibits HNMT activity on the μM order of IC 50 . Chirality is important, and (M)-isomers exhibits substantially reduced activity. The 6-iodo group is also essential, which suggests the involvement of halogen bonds in protein binding. Substituents on the sulfonate moiety also affect the inhibitory activity.

本文言語英語
ページ(範囲)476-481
ページ数6
ジャーナルJournal of Antibiotics
72
6
DOI
出版ステータス出版済み - 6月 1 2019
外部発表はい

!!!All Science Journal Classification (ASJC) codes

  • 薬理学
  • 創薬

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