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

M Arisawa, Y Kasaya, T Obata, T Sasaki…

Index: Arisawa, Mitsuhiro; Kasaya, Yayoi; Obata, Tohru; Sasaki, Takuma; Nakamura, Tomonori; Araki, Takuya; Yamamoto, Koujirou; Sasaki, Akito; Yamano, Akihito; Ito, Mika; Abe, Hiroshi; Ito, Yoshihiro; Shuto, Satoshi Journal of Medicinal Chemistry, 2012 , vol. 55, # 18 p. 8152 - 8163

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Citation Number: 14

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.

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Synthesis of indomethacin analogues for evaluation as modula...

[Maguire, Anita R.; Plunkett, Stephen J.; Papot, Sebastien; Clynes, Martin; O'Connor, Robert; Touhey, Samantha Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 3 p. 745 - 762]

Design and synthesis of indomethacin analogues that inhibit ...

[Arisawa, Mitsuhiro; Kasaya, Yayoi; Obata, Tohru; Sasaki, Takuma; Ito, Mika; Abe, Hiroshi; Ito, Yoshihiro; Yamano, Akihito; Shuto, Satoshi ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 5 p. 353 - 357]