Design and Synthesis of Indomethacin Analogues That Inhibit P-Glycoprotein and/or Multidrug Resistant Protein without Cox Inhibitory Activity

作者：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

来源：Journal of Medicinal Chemistry, 2012, 55(18): 8152-8163.

DOI：10.1021/jm301084z

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.

• 出版日期2012-9-27