Nitrohydroxyquinoline derivative and preparation method and application thereof
The invention discloses a nitrohydroxyquinoline derivative and a preparation method and application thereof. Specifically, the invention discloses a compound shown as a general formula (I), a preparation method of the compound, a pharmaceutical composition containing the compound, and an application of the compound in treatment on infectious diseases or cancers. The compound disclosed by the invention has different anti-tumor activities and can be developed into a medicine for treating tumors. The definition of each group in the general formula (I) is the same as that in the specification.
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Paragraph 0259-0262
(2020/12/05)
Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases
There is interest in developing potent, selective, and cell-permeable inhibitors of human ferrous iron and 2-oxoglutarate (2OG) oxygenases for use in functional and target validation studies. The 3-component Betti reaction enables efficient one-step C-7 functionalisation of modified 8-hydroxyquinolines (8HQs) to produce cell-active inhibitors of KDM4 histone demethylases and other 2OG oxygenases; the work exemplifies how a template-based metallo-enzyme inhibitor approach can be used to give biologically active compounds.
Quinoline synthesis by improved Skraup-Doebner-Von Miller reactions utilizing acrolein diethyl acetal
A robust synthetic method has been developed as an improvement to the venerable Skraup-Doebner-Von Miller reaction providing access to various quinoline products. The straightforward procedure utilizes acrolein diethyl acetal as a three-carbon annulation partner with aniline substrates in a monophasic, organic solvent-free reaction medium. Differentially substituted aniline precursors were found to be compatible with the reaction conditions and the corresponding quinoline products are isolated in moderate to good yields.
Ramann, Ginelle A.,Cowen, Bryan J.
supporting information
p. 6436 - 6439
(2015/11/16)
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