- Effect of 3-subsitution of quinolinehydroxamic acids on selectivity of histone deacetylase isoforms
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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
- Mehndiratta, Samir,Chen, Mei-Chuan,Chao, Yuh-Hsuan,Lee, Cheng-Hsin,Liou, Jing-Ping,Lai, Mei-Jung,Lee, Hsueh-Yun
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- PHENANTHROLINE PHOSPHONIC ACID DERIVATIVE AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
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The present invention relates to a novel phenanthroline phosphonic acid compound and a pharmaceutical salt thereof, as well as an application of the compound and the pharmaceutical salt thereof as collagen prolyl hydroxylase inhibitors in the preparation of drugs for preventing or treating collagen prolyl-4-hydroxylase related disease.
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Paragraph 0093-0095
(2017/02/28)
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- 5-Position-selective C-H trifluoromethylation of 8-aminoquinoline derivatives
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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.
- Kuninobu, Yoichiro,Nishi, Mitsumi,Kanai, Motomu
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supporting information
p. 8092 - 8100
(2016/09/09)
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- QUINOLINE DERIVATIVES FOR DIAGNOSIS AND TREATMENT OF ALZHEIMER'S DISEASE
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A new class of quinoline compounds is useful for the detection and treatment of Alzheimer's disease and other neurodegenerative diseases such as amyloidoses and tauopathies. The compounds can be synthesized in radiolabeled form for use as imaging agents,
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Page/Page column 12
(2016/11/28)
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- Synthesis and structure activity relationship of 3-(arylsulfonyl)-8- (piperidin-4-yl amino)quinoline derivatives as 5-HT6 receptor antagonists
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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.
- Nirogi, Ramakrishna V.S.,Badange, Rajeshkumar,Gudla, Parandhama,Khagga, Mukkanti
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p. 3779 - 3784
(2014/08/05)
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- NITROGEN-CONTAINING HETEROARYL COMPOUNDS HAVING HIV INTEGRASE INHIBITORY ACTIVITY
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A compound of the formula (I): wherein Z4, Z5 and Z9 each is independently carbon atom or nitrogen atom; Y is hydroxy, mercapto or amino; RA is a group of the formula: (wherein C ring is nitrogen-containing heteroaryl) has an inhibitory activity against integrase.
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Page 114; 115
(2008/06/13)
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- Improved Syntheses of Some Monohloro- and Monobromo-8-quinolinols
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Procedures were developed for the preparation of the 2-, 3-, 4-, and 6-monosubstituted chloro and bromo 8-quinolinols which afforded greater yields and/or reduced the number of steps in the preparation. 100 MHz 1H-NMR spetra for the 12 possible monochloro
- Gershon, Herman,Clarke, Donald D.
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p. 935 - 942
(2007/10/02)
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