Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
Basic Information
ID: ALA4052700
Journal: Bioorg Med Chem
Title: Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.
Authors: Pan M, Cui J, Jiao L, Ghaleb H, Liao C, Zhou J, Kairuki M, Lin H, Huang W, Qian H.
Abstract: 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.
CiteXplore: 28645831
DOI: 10.1016/j.bmc.2017.06.015
Patent ID: ┄