期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 63, 期 10, 页码 5458-5476出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.0c00337
关键词
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资金
- National Natural Science Foundation of China [81803358, 81703329, 81273364, 81773114]
- Nonprofit Central Research Institute of Chinese Academy of Medical Sciences [2019-RC-HL-008]
SIS3 is a specific inhibitor of Smad3 that inhibits the TGF beta 1-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 aided by late-stage functionalization of a 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 P-gp.
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