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Discovery of Potent Inhibitors against P-Glycoprotein-Mediated Multidrug Resistance Aided by Late-Stage Functionalization of a 2-(4-(Pyridin-2-yl)phenoxy)pyridine Analogue by Ma, Yao; Yin, Dawei; Ye, Jingjia; Wei, Xiduan; Pei, Yameng; Li, Xueyuan; Si, Guangxu; Chen, Xuan-Yu; Chen, Zhe-sheng; Dong, Yi; Zou, Feng; Shi, Wei; Qiu, Qianqian; Qian, Hai; Liu, Gang is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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SIS3 is a specific inhibitor of Smad3 that inhibits the TGFβ1-induced phosphorylation of Smad3. In this article, a variety of SIS3 derivatives were designed and synthesized to discover potential inhibitors against P-glycoprotein-mediated multidrug resistance to cancer cells aided by late-stage functionalization of 2-(4-(pyridin-2-yl)phenoxy)pyridine analogue. A novel class of potent P-gp reversal agents were investigated and a lead compound 37 was identified as a potent P-gp reversal agent with strong bioactivity and outstanding affinity for ABCB1.

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Author

Ma, Yao; Yin, Dawei; Ye, Jingjia; Wei, Xiduan; Pei, Yameng; Li, Xueyuan; Si, Guangxu; Chen, Xuan-Yu; Chen, Zhe-sheng; Dong, Yi; Zou, Feng; Shi, Wei; Qiu, Qianqian; Qian, Hai; Liu, Gang

Publisher

American Chemical Society; American Chemical Society (ACS) (ISSN 0022-2623)

Published

2020

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)