期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 25, 期 15, 页码 4194-4202出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.06.015
关键词
ABCB1 inhibitors; MDR; P-glycoprotein; Cancer resistance
资金
- National Natural Science Foundation of China [81370878, 81673299]
- '333' Project of Jiangsu Province [BRA2015393]
- National Science and Technology Major Project of the Ministry of Science and Technology of China [2009ZX09102-033]
Cancer chemotherapy failure is often due to the overexpression of ATP-binding cassette (ABC) transporters (particularly ABCB1), resulting in a variety of structurally and pharmacologically unrelated drugs efflux. The multidrug resistance (MDR) phenomenon could be reversed by ABCB1 inhibitors. Now, JL-A7 as the lead compound based on a triazol-N-ethyl-tetrahydroisoquinoline scaffold, 18 compounds were designed and synthesized. Substitution in para positions yielded high activities toward ABCB1. Moreover, compound 5 could effectively block the drug efflux function of ABCB1 and increase the accumulation of anti-cancer drugs to achieve effective treatment concentration in MDR cells. (C) 2017 Elsevier Ltd. All rights reserved.
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