Abstract:Fused tetracyclic systems containing a quinoline nucleus represent an important class of heterocyclic bioactive natural products and pharmaceuticals because of their significant and wide-spectrum biological properties.
“…For decades, quinoline derivatives have been useful in various anticancer drug applications. For example, neratinib ( I ) is used to treat breast cancer [ 2 ]; pelitinib ( II ) has irreversible EGFR inhibitory activity [ 3 ]; bosutinib ( III ) is used to treat chronic myelogenous leukemia [ 4 ]; cabozantinib ( IV ) and lenvatinib ( V ) are used to treat medullary thyroid anticancer [ 5 , 6 ]; and topotecan ( VI ) is used to treat cancer of the ovaries and certain types of lung cancers [ 7 , 8 ] ( Figure 1 ). Figure 1 Certain anticancer drug structures of quinoline derivatives I-VI and the structure of newly synthesized compounds 5–17 .…”
Tetrahydroquinoline (THQ) is an important structure for synthesizing multiple biologically active derivatives. Thus, we developed new quinoline derivatives and investigated them as anticancer agents. First, infrared spectroscopy, nuclear magnetic resonance spectroscopy, and other techniques were used to confirm the structure of synthesized compounds. Then, they were assessed in vitro against three human cancer cell lines. Consequently, four compounds, 10, 13, 15, and 16, were identified as promising anticancer agents with pyrazolo quinoline derivative (15) exhibiting the highest potential IC 50 and a strong apoptotic effect on three cell lines.
“…For decades, quinoline derivatives have been useful in various anticancer drug applications. For example, neratinib ( I ) is used to treat breast cancer [ 2 ]; pelitinib ( II ) has irreversible EGFR inhibitory activity [ 3 ]; bosutinib ( III ) is used to treat chronic myelogenous leukemia [ 4 ]; cabozantinib ( IV ) and lenvatinib ( V ) are used to treat medullary thyroid anticancer [ 5 , 6 ]; and topotecan ( VI ) is used to treat cancer of the ovaries and certain types of lung cancers [ 7 , 8 ] ( Figure 1 ). Figure 1 Certain anticancer drug structures of quinoline derivatives I-VI and the structure of newly synthesized compounds 5–17 .…”
Tetrahydroquinoline (THQ) is an important structure for synthesizing multiple biologically active derivatives. Thus, we developed new quinoline derivatives and investigated them as anticancer agents. First, infrared spectroscopy, nuclear magnetic resonance spectroscopy, and other techniques were used to confirm the structure of synthesized compounds. Then, they were assessed in vitro against three human cancer cell lines. Consequently, four compounds, 10, 13, 15, and 16, were identified as promising anticancer agents with pyrazolo quinoline derivative (15) exhibiting the highest potential IC 50 and a strong apoptotic effect on three cell lines.
“…Cascade enzyme reactions have been utilized with different purposes, especially in the development of a more-efficient synthesis of chemical compounds, such as bioactive oligosaccharides, glycosylated molecules, or amoniacid derivatives [21][22][23][24][25][26].…”
Cascade reactions have been described as efficient and universal tools, and are of substantial interest in synthetic organic chemistry. This review article provides an overview of the novel and recent achievements in enzyme cascade processes catalyzed by multi-enzymatic or chemoenzymatic systems. The examples here selected collect the advances related to the application of the sequential use of enzymes in natural or genetically modified combination; second, the important combination of enzymes and metal complex systems, and finally we described the application of biocatalytic biohybrid systems on in situ catalytic solid-phase as a novel strategy. Examples of efficient and interesting enzymatic catalytic cascade processes in organic chemistry, in the production of important industrial products, such as the designing of novel biosensors or bio-chemocatalytic systems for medicinal chemistry application, are discussed
“…Currently, many quinoline-containing drugs are available on the market [ 3 , 4 ]. Recently, three protein kinase inhibitors (Lenvatinib, Bosutinib, and Cabozantinib) and one Farnesyl transferase inhibitor (Tipifarnib) were presented as anticancer agents [ 5 ].…”
Section: Introductionmentioning
confidence: 99%
“…Currently, many quinoline-containing drugs are available on the market [3,4]. Recently, three 4a-6a = X = N-Ph, obtained from 2; 4b-6b = X = O, obtained from 3; 9a and 10a: R 1 = R 2 = R 3 = H, 10b: R 1 = H, R 2 = Cl, R 3 = H, 10c: R 1 = H, R 2 = R 3 = Cl, 10d: R 1 = Me, R 2 = H, R 3 = H, 10e: R 1 = Me, R 2 = R 3 = Cl, 10f: R 1 = H, R 2 = R 3 = I, 11a:…”
A series of 1,3,4-oxadiazole bridged pyrazole/isoxazole bearing quinoline derivatives has been designed and synthesized by a clean and convenient method. Structures of the newly synthesized compounds have been confirmed by FTIR,
1
H and
13
C NMR, and HRMS spectral data. The titled compounds have been evaluated for their molecular docking guided antimicrobial and anti-inflammatory activity. One of 1,3,4-oxadiazole bridged quinolinyl-pyrazole derivatives has interacted efficiently with
E. Coli
protein (PDB file: 1KZN), and has been characterized by good antimicrobial activity against the majority of the tested pathogens. Another product has exhibited excellent anti-inflammatory activity.
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