A Selective and Orally Bioavailable Quinoline-6-Carbonitrile-Based Inhibitor of CDK8/19 Mediator Kinase with Tumor-Enriched Pharmacokinetics
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
Chen, Mengqian,Cheng, Chen,Chumanevich, Alexander A.,Gorbunova, Svetlana,Li, Jing,McInnes, Campbell,Mindich, Aleksei,Porter, Donald C.,Roninson, Igor B.,Wang, Lili,Zhang, Li
supporting information
(2022/02/16)
Direct C-3-alkenylation of quinolones via palladium-catalyzed C-H functionalization
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
supporting information; experimental part
p. 2445 - 2449
(2010/12/25)
Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities
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
p. 1015 - 1018
(2007/10/03)
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