49713-51-1Relevant articles and documents
A Selective and Orally Bioavailable Quinoline-6-Carbonitrile-Based Inhibitor of CDK8/19 Mediator Kinase with Tumor-Enriched Pharmacokinetics
Zhang, Li,Cheng, Chen,Li, Jing,Wang, Lili,Chumanevich, Alexander A.,Porter, Donald C.,Mindich, Aleksei,Gorbunova, Svetlana,Roninson, Igor B.,Chen, Mengqian,McInnes, Campbell
supporting information, p. 3420 - 3433 (2022/02/16)
Senexins are potent and selective quinazoline inhibitors of CDK8/19 Mediator kinases. To improve their potency and metabolic stability, quinoline-based derivatives were designed through a structure-guided strategy based on the simulated drug–target dockin
QUINOLINE-BASED COMPOUNDS AND METHODS OF INHIBITING CDK8/19
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Paragraph 0108; 0110-0111; 0115, (2020/03/09)
Disclosed herein are quinoline-based compounds and method for inhibiting CDK8 or CDK19 for the intervention in diseases, disorders, and conditions. The quinoline-based composition comprise substituents at quinoline ring positions 4 and 6, wherein the substituent at position 4 is selected from a substituted or unsubstituted arylalkylamine or a substituted or unsubstituted arylhetrocyclylamine. Pharmaceutical compositions comprising the substituted qunioline compositions, methods of inhibiting CDK8 or CDK19, and methods of treating CDK8/19-associated diseases, disorders, or conditions are also disclosed.
Oxidation method of 4-oxo-2,3-dihydroquinoline compound
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Paragraph 0018, (2018/12/05)
The invention discloses an oxidation method of a 4-oxo-2,3-dihydroquinoline compound. The method comprises the following steps: taking the 4-oxo-2,3-dihydroquinoline compound as a raw material; addingan organic solvent, an acidifying agent and an oxidizing agent; performing oxidation reaction at 50-85 DEG C; and after the reaction is finished, performing post-treatment on the reaction liquid to obtain a 4-hydroxyquinoline compound. Various raw materials used by the preparation method disclosed by the invention are simple and easy to obtain, are industrial products and have wide sources and low price; the preparation method is simple, easy to operate and high in product yield; compared with the traditional oxidation method of the 4-oxo-2,3-dihydroquinoline compound, the method disclosed bythe invention has the advantages of being more efficient and simpler in post-treatment; and the method is especially important for the industrialization of the product.