Structure-activity relationship of novel menaquinone-4 analogues: Modification of the side chain affects their biological activities

Yoshitomo Suhara, Norika Hanada, Takashi Okitsu, Miho Sakai, Masato Watanabe, Kimie Nakagawa, Akimori Wada, Kazuyoshi Takeda, Kazuhiko Takahashi, Hiroaki Tokiwa, Toshio Okano

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

We synthesized new vitamin K analogues with demethylation or reduction of the double bonds of the side chain of menaquinone-4 (MK-4) and evaluated their SXR-mediated transcriptional activity as well as the extent of their conversion to MK-4. The results indicated that the analogue with the methyl group deleted at the 7′ site of the side chain part affected conversion activity to MK-4. In contrast, a decrease in the number of the double bonds in the side chain moiety appeared to decrease the SXR-mediated transcriptional activity.

Original languageEnglish
Pages (from-to)1553-1558
Number of pages6
JournalJournal of Medicinal Chemistry
Volume55
Issue number4
DOIs
Publication statusPublished - 2012 Feb 23

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    Suhara, Y., Hanada, N., Okitsu, T., Sakai, M., Watanabe, M., Nakagawa, K., Wada, A., Takeda, K., Takahashi, K., Tokiwa, H., & Okano, T. (2012). Structure-activity relationship of novel menaquinone-4 analogues: Modification of the side chain affects their biological activities. Journal of Medicinal Chemistry, 55(4), 1553-1558. https://doi.org/10.1021/jm2013166