137105-06-7Relevant academic research and scientific papers
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.
Copper-catalysed heteroannulation with alkynes: A general and highly regio- and stereoselective method for the synthesis of (E)-2-(2-arylvinyl) quinazolinones
Kundu, Nitya G,Chaudhuri, Gopeswar
, p. 6833 - 6842 (2007/10/03)
A highly regio- and stereoselective procedure for the synthesis of 2-substituted-1,2,3,4-tetrahydroquinazolinones through a two-step procedure, e.g. (i) palladium-copper catalysed C-arylation of terminal alkynes and (ii) copper-catalysed cyclisation of di
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
Synthesis and structure-activity relationships of N-substituted 2-[(2-imidazolylsulfinyl)methyl]anilines as a new class of gastric H+/K+-ATPase inhibitors
Yamakawa,Matsukura,Nomura,Yoshioka,Masaki,Igata,Okabe
, p. 1746 - 1752 (2007/10/02)
A series of N-substituted 2-[(2-imidazolylsulfinyl)methyl]anilines was synthesized and evaluated for its biological activity against H+/K+-ATPase prepared from rabbit stomach and gastric acid secretions in Heidenhain pouch dogs. Monoalkyl substituents on the nitrogen atom of the aniline moiety markedly inhibited the enzyme activity to the same degree as omeprazole, a representative H+/K+-ATPase inhibitor. Most of these compounds, administered at 3 mg/kg i.v. inhibited histamine-stimulated gastric acid secretion. The inhibitory activity of these derivatives on the enzymes at pH 6.0 was more potent than that at pH 7.4, and was distinctly correlated to stability in aqueous solution at pH 5.0.
