137105-06-7Relevant articles and documents
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as P-glycoprotein-mediated multidrug resistance inhibitors
Gao, Yang,Shi, Wei,Cui, Jian,Liu, Chunxia,Bi, Xinzhou,Li, Zhuo,Huang, Wenlong,Wang, Guangji,Qian, Hai
supporting information, p. 2420 - 2427 (2018/04/10)
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.
A highly regio- And stereoselective synthesis of (Z)-3-arylidene-2,3-dihydro-5H-1,4-benzodioxepin-5-ones and (Z)-3-arylidene1,2,3,5-tetrahydro-4,1-benzoxazepin-5-ones through palladium-copper catalysis
Chaudhuri, Gopeswar,Kundu, Nitya G.
, p. 775 - 779 (2007/10/03)
Sodium 2-(prop-2′-ynyloxy)benzoate 1a reacted with the aryl iodides 2-10 in the presence of bis(triphenylphosphine)palladium(II) chloride, cuprous iodide and triethylamine in CH3CN-DMF to yield the disubstituted alkynes 11-19 in good yields (48
