期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 26, 期 9, 页码 2420-2427出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2018.03.045
关键词
Cancer; Multidrug resistance; P-glycoprotein; Reversal agents
资金
- National Science Foundation of China [81673299]
- National Science and Technology Major Project of the Ministry of Science and Technology of China [2009ZX09102-033]
Multidrug resistance (MDR) is one of the main obstacles of clinical chemotherapy. A great deal of research shows that the occurrence of drug resistance in various malignant tumors is closely related to the expression of P-glycoprotein (P-gp) on the surface of the cell membrane. In this paper, based on the structure-activity relationship of phenylethyl tetrahydroisoquinoline, we choose tariquidar as the lead compound for the design and synthesis of 17 novel tetrahydroisoquinoline P-gp inhibitors. Additionally, in vitro and in vivo cytotoxicity assays and reversed MDR activity assays were evaluated. Among them, compound 3 had a good reversal of MDR activity and the reversal mechanism study of it was carried out. All of these results demonstrated that compound 3 was considered to be a promising P-gp-mediated MDR reversal candidate. (C) 2018 Elsevier Ltd. All rights reserved.
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