5341-07-1Relevant articles and documents
Effect of 3-subsitution of quinolinehydroxamic acids on selectivity of histone deacetylase isoforms
Mehndiratta, Samir,Chen, Mei-Chuan,Chao, Yuh-Hsuan,Lee, Cheng-Hsin,Liou, Jing-Ping,Lai, Mei-Jung,Lee, Hsueh-Yun
, p. 74 - 84 (2020/11/10)
A series of 3-subsituted quinolinehydroxamic acids has been synthesised and evaluated for their effect on human lung cancer cell line (A549), human colorectal cancer cell line (HCT116) and HDAC isoforms 1, 2, 6, and 8. The results indicated that substitut
5-Position-selective C-H trifluoromethylation of 8-aminoquinoline derivatives
Kuninobu, Yoichiro,Nishi, Mitsumi,Kanai, Motomu
supporting information, p. 8092 - 8100 (2016/09/09)
We developed a copper-catalyzed 5-position-selective C-H trifluoromethylation of 8-aminoquinoline derivatives. The reaction proceeded with high functional group tolerance under mild conditions. In the case of quinolines with an amide, carbamate, urea, or sulfonamide group at the 8-position of quinoline moieties, a radical scavenger experiment indicated that the reaction proceeded via a radical pathway. The protecting group of an 8-amidoquinoline derivative could be removed by hydrolysis. On the other hand, the trifluoromethylation of 8-aminoquinolines was also promoted by other Lewis acids as well as a copper catalyst and proceeded even in the presence of a radical scavenger. These results indicated that the trifluoromethylation of 8-aminoquinolines proceeded via a Friedel-Crafts-type reaction. Interestingly, the copper salt works as either a catalyst for the formation of a CF3 radical or a Lewis acid to promote a Friedel-Crafts-type reaction, depending on the substrate.
Synthesis and structure activity relationship of 3-(arylsulfonyl)-8- (piperidin-4-yl amino)quinoline derivatives as 5-HT6 receptor antagonists
Nirogi, Ramakrishna V.S.,Badange, Rajeshkumar,Gudla, Parandhama,Khagga, Mukkanti
, p. 3779 - 3784 (2014/08/05)
As part of our efforts to develop better therapies for the treatment of cognitive impairment associated with Alzheimer's disease and Schizophrenia, we have focused our research towards 5-HT6 receptor (5-HT6R) in order to identify potent and selective ligands for this purpose. Herein, we report the synthesis, structure activity relationship and biological evaluation of a novel series of 3-(arylsulfonyl)-8- (piperidin-4-yl amino)quinoline derivatives, as 5-HT6 receptor (5-HT6R) antagonists. In this work, we have shown that moving from aryl sulfonamide platform to biaryl sulfone platform retains the 5-HT6.R affinity when tested in vitro in cell based reporter gene functional assay.