Design and Synthesis of Indomethacin Analogues That Inhibit P-Glycoprotein and/or Multidrug Resistant Protein without Cox Inhibitory Activity
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- 作者：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
- 刊名：Journal of Medicinal Chemistry
- 出版年：2012
- 出版时间：September 27, 2012
- 年：2012
- 卷：55
- 期：18
- 页码：8152-8163
- 全文大小：577K
- 年卷期：v.55,no.18(September 27, 2012)
- ISSN：1520-4804
文摘
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.