- A Selective and Orally Bioavailable Quinoline-6-Carbonitrile-Based Inhibitor of CDK8/19 Mediator Kinase with Tumor-Enriched Pharmacokinetics
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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
- 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
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supporting information
p. 3420 - 3433
(2022/02/16)
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- Cu(I)-Catalyzed Alkynylation of Quinolones
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Herein we report the first alkynylation of quinolones with terminal alkynes under mild reaction conditions. The reaction is catalyzed by Cu(I) salts in the presence of a Lewis acid, which is essential for the reactivity of the system. The enantioselective version of this transformation has also been explored, and the methodology has been applied in the synthesis of the enantioenriched tetrahydroquinoline alkaloid cuspareine.
- Maestro, Aitor,Lemaire, Sebastien,Harutyunyan, Syuzanna R.
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supporting information
p. 1228 - 1231
(2022/02/14)
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- QUINOLINE-BASED COMPOUNDS AND METHODS OF INHIBITING CDK8/19
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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.
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Paragraph 0108; 0110-0111; 0115
(2020/03/09)
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- Highly Enantioselective Catalytic Addition of Grignard Reagents to N-Heterocyclic Acceptors
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General methods to prepare chiral N-heterocyclic molecular scaffolds are greatly sought after because of their significance in medicinal chemistry. Described here is the first general catalytic methodology to access a wide variety of chiral 2- and 4-substituted tetrahydro-quinolones, dihydro-4-pyridones, and piperidones with excellent yields and enantioselectivities, utilizing a single catalyst system.
- Guo, Yafei,Harutyunyan, Syuzanna R.
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supporting information
p. 12950 - 12954
(2019/08/07)
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- Oxidation method of 4-oxo-2,3-dihydroquinoline compound
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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.
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Paragraph 0018
(2018/12/05)
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- Structural optimization of quinolon-4(1 H)-imines as dual-stage antimalarials: Toward increased potency and metabolic stability
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Discovery of novel effective and safe antimalarials has been traditionally focused on targeting erythrocytic parasite stages that cause clinical symptoms. However, elimination of malaria parasites from the human population will be facilitated by intervent
- Ressurrei??o, Ana S.,Gon?alves, Daniel,Sitoe, Ana R.,Albuquerque, Ine?s S.,Gut, Jiri,Góis, Ana,Gon?alves, Lídia M.,Bronze, Maria R.,Hanscheid, Thomas,Biagini, Giancarlo A.,Rosenthal, Philip J.,Prude?ncio, Miguel,O'Neill, Paul,Mota, Maria M.,Lopes, Francisca,Moreira, Rui
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p. 7679 - 7690
(2013/11/06)
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- Direct C-3-alkenylation of quinolones via palladium-catalyzed C-H functionalization
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An unprecedented C-3-alkenylation of quinolones was reported through palladium-catalyzed C-H functionalization with 1% catalyst loading. This method provides an efficient route to a variety of new quinolone derivatives.
- Li, Mingzong,Li, Liangxi,Ge, Haibo
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supporting information; experimental part
p. 2445 - 2449
(2010/12/25)
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- Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities
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A simple two-step synthesis method was used to make 51 B-ring-substituted 4-hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth of chloroquine sensitive and resistant strains of Plasmodium falciparum, the dominant cause of malaria morbidity. Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2.
- Madrid, Peter B.,Sherrill, John,Liou, Ally P.,Weisman, Jennifer L.,DeRisi, Joseph L.,Guy, R. Kiplin
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p. 1015 - 1018
(2007/10/03)
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- Pyrido [1,2,3-DE]quinoxaline derivatives, process for their production and their use in pharmaceutical agents
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Pyrido[1,2,3-de]quinoxaline derivatives of formula I STR1 in which R 1, R 2 and R 3 each mean hydrogen, --POXY, halogen or --COR,R 4 means hydrogen or OH,R 5, R 6 and R 7 are the same or different and mean hydrogen, halogen, nitro, NR 12 R 13, cyano, CF 3, C 1-6 alkyl, C 1-4 alkoxy, orR 5 and R 6 or R 6 and R 7 represent a fused benzene ring, and means a single or double bond,are described as well as their production and use in pharmaceutical agents.
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