Design and synthesis of indomethacin analogues that inhibit P-glycoprotein and/or multidrug resistant protein without Cox inhibitory activity

Mitsuhiro Arisawa, Yayoi Kasaya, Tohru Obata, Takuma Sasaki, Tomonori Nakamura, Takuya Araki, Koujirou Yamamoto, Akito Sasaki, Akihito Yamano, Mika Ito, Hiroshi Abe, Yoshihiro Ito, Satoshi Shuto

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Abstract

We designed and synthesized conformationally restricted analogues and regioisomers of the nonsteroidal anti-inflammatory drug indomethacin. Evaluation of the inhibitory effects of these compounds on COX, P-glycoprotein, and multidrug resistance indicated that NSAIDS modulation of multidrug-resistant P-glycoprotein and multidrug-resistant protein-1 is not associated with COX-1 and COX-2 inhibitory activities.

Original languageEnglish
Pages (from-to)8152-8163
Number of pages12
JournalJournal of Medicinal Chemistry
Volume55
Issue number18
DOIs
Publication statusPublished - 2012 Sep 27
Externally publishedYes

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Arisawa, M., Kasaya, Y., Obata, T., Sasaki, T., Nakamura, T., Araki, T., Yamamoto, K., Sasaki, A., Yamano, A., Ito, M., Abe, H., Ito, Y., & Shuto, S. (2012). Design and synthesis of indomethacin analogues that inhibit P-glycoprotein and/or multidrug resistant protein without Cox inhibitory activity. Journal of Medicinal Chemistry, 55(18), 8152-8163. https://doi.org/10.1021/jm301084z