Synthesis and biological assessment of indole derivatives containing penta-heterocycles scaffold as novel anticancer agents towards A549 and K562 cells

Zhang, Guanglong; Tang, Zhengyi; Fan, Sili; Li, Chengpeng; Li, Yan; Liu, Weiqin; Long, Xuesha; Zhang, Wenjing; Zhang, Yi; Li, Zhurui; Wang, Zhenchao; Chen, Danping; Ouyang, Gangfeng

doi:10.1080/14756366.2022.2163393

Cited by 11 publications

(5 citation statements)

References 50 publications

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“…To investigate whether the cell growth inhibition was associated with apoptosis, the plant pathogenic bacterial cells were treated with either DMSO or various concentrations of the target compound for 15 h using previous reported methods with slight modifications [ 38 , 39 ]. After treatment with different concentrations of 6e (0, 1 × EC 50 , 2 × EC 50 , and 5 × EC 50 ), the cells were washed twice with cold PBS, centrifuged, and collected.…”

Section: Methodsmentioning

confidence: 99%

Discovery and Mechanism of Novel 7-Aliphatic Amine Tryptanthrin Derivatives against Phytopathogenic Bacteria

Long

Zhang

Long

et al. 2023

IJMS

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Rice bacterial leaf blight is a destructive bacterial disease caused by Xanthomonas oryzae pv. oryzae (Xoo) that seriously threatens crop yields and their associated economic benefits. In this study, a series of improved dissolubility 7-aliphatic amine tryptanthrin derivatives was designed and synthesized, and their potency in antibacterial applications was investigated. Notably, compound 6e exhibited excellent activity against Xoo, with an EC50 value of 2.55 μg/mL, compared with the positive control bismerthiazol (EC50 = 35.0 μg/mL) and thiodiazole copper (EC50 = 79.4 μg/mL). In vivo assays demonstrated that 6e exhibited a significant protective effect on rice leaves. After exposure, the morphology of the bacteria was partially atrophied by SEM. Furthermore, 6e increased the accumulation of intracellular reactive oxygen species, causing cell apoptosis and the formation of bacterial biofilms. All the results indicated that 6e could be a potential agrochemical bactericide for controlling phytopathogenic bacteria.

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Section: Methodsmentioning

confidence: 99%

Discovery and Mechanism of Novel 7-Aliphatic Amine Tryptanthrin Derivatives against Phytopathogenic Bacteria

Long

Zhang

Long

et al. 2023

IJMS

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“…The morphology changes of Xac bacteria, intracellular ROS accumulation, apoptotic ratio, and growth curves assays after incubation with 7c were performed according to previous literature. – …”

Section: Methodsmentioning

confidence: 99%

Design, Synthesis, and Mechanism of Novel 9-Aliphatic Amine Tryptanthrin Derivatives against Phytopathogenic Bacteria

Zhang,

Li,

et al. 2023

J. Agric. Food Chem.

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“…The MTT proliferation test on the epithelial cell line HEK293 was performed as pre-viously described [ 39 ]. The 50% inhibiting concentrations (IC 50 ) were determined by linear regression analysis.…”

Section: Methodsmentioning

confidence: 99%

New 2,4-bis[(substituted-aminomethyl)phenyl]phenylquinazoline and 2,4-bis[(substituted-aminomethyl)phenyl]phenylquinoline Derivatives: Synthesis and Biological Evaluation as Novel Anticancer Agents by Targeting G-Quadruplex

Guillon,

Le Borgne,

Milano

et al. 2023

Pharmaceuticals

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The syntheses of novel 2,4-bis[(substituted-aminomethyl)phenyl]phenylquinazolines 12 and 2,4-bis[(substituted-aminomethyl)phenyl]phenylquinolines 13 are reported here in six steps starting from various halogeno-quinazoline-2,4-(1H,3H)-diones or substituted anilines. The antiproliferative activities of the products were determined in vitro against a panel of breast (MCF-7 and MDA-MB-231), human adherent cervical (HeLa and SiHa), and ovarian (A2780) cell lines. Disubstituted 6- and 7-phenyl-bis(3-dimethylaminopropyl)aminomethylphenyl-quinazolines 12b, 12f, and 12i displayed the most interesting antiproliferative activities against six human cancer cell lines. In the series of quinoline derivatives, 6-phenyl-bis(3-dimethylaminopropyl)aminomethylphenylquinoline 13a proved to be the most active. G-quadruplexes (G4) stacked non-canonical nucleic acid structures found in specific G-rich DNA, or RNA sequences in the human genome are considered as potential targets for the development of anticancer agents. Then, as small aza-organic heterocyclic derivatives are well known to target and stabilize G4 structures, their ability to bind G4 structures have been determined through FRET melting, circular dichroism, and native mass spectrometry assays. Finally, telomerase inhibition ability has been also assessed using the MCF-7 cell line.

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Synthesis and biological assessment of indole derivatives containing penta-heterocycles scaffold as novel anticancer agents towards A549 and K562 cells

Cited by 11 publications

References 50 publications

Discovery and Mechanism of Novel 7-Aliphatic Amine Tryptanthrin Derivatives against Phytopathogenic Bacteria

Discovery and Mechanism of Novel 7-Aliphatic Amine Tryptanthrin Derivatives against Phytopathogenic Bacteria

Design, Synthesis, and Mechanism of Novel 9-Aliphatic Amine Tryptanthrin Derivatives against Phytopathogenic Bacteria

New 2,4-bis[(substituted-aminomethyl)phenyl]phenylquinazoline and 2,4-bis[(substituted-aminomethyl)phenyl]phenylquinoline Derivatives: Synthesis and Biological Evaluation as Novel Anticancer Agents by Targeting G-Quadruplex

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