Novel N-4-piperazinyl-ciprofloxacin-chalcone hybrids: Synthesis, physicochemical properties, anticancer and topoisomerase I and II inhibitory activity

Abdel‐Aziz, Mohamed; Park, So Eun; Abuo‐Rahma, Gamal El‐Din A.; Sayed, Mohamed; Kwon, Young Joo

doi:10.1016/j.ejmech.2013.08.040

Cited by 107 publications

(52 citation statements)

References 33 publications

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“…Compounds 101a , 101d , 101e , 101g , 101j were selected for in vitro anticancer screening performed by the National Cancer Institute against 60 cell lines from 9 tumor subpanels, including leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, and breast cell lines. Hybrid 101a exhibited the highest broad-spectrum antitumor activity, while 101g revealed selectivity towards the leukemia subpanel [179] (Fig. 24).…”

Section: Other Modificationsmentioning

confidence: 99%

Modifications of quinolones and fluoroquinolones: hybrid compounds and dual-action molecules

Fedorowicz

Sączewski

2018

Monatsh Chem

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This review is aimed to provide extensive survey of quinolones and fluoroquinolones for a variety of applications ranging from metal complexes and nanoparticle development to hybrid conjugates with therapeutic uses. The review covers the literature from the past 10 years with emphasis placed on new applications and mechanisms of pharmacological action of quinolone derivatives. The following are considered: metal complexes, nanoparticles and nanodrugs, polymers, proteins and peptides, NO donors and analogs, anionic compounds, siderophores, phosphonates, and prodrugs with enhanced lipophilicity, phototherapeutics, fluorescent compounds, triazoles, hybrid drugs, bis-quinolones, and other modifications. This review provides a comprehensive resource, summarizing a broad range of important quinolone applications with great utility as a resource concerning both chemical modifications and also novel hybrid bifunctional therapeutic agents.Graphical abstract

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Section: Other Modificationsmentioning

confidence: 99%

Modifications of quinolones and fluoroquinolones: hybrid compounds and dual-action molecules

Fedorowicz

Sączewski

2018

Monatsh Chem

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“…[37,38,43,44] The appropriate intermediate 4a-e (0.001 mol) in a mixture with ciprofloxacin (0.331 g, 0.001 mol) and triethyamine (0.202 g, 0.002 mol) in acetonitrile (10 mL) were heated at reflux for 7-8 h. The formed precipitate was filtered off while hot, washed with acetonitrile and dried. [17 ] 4. 1.1.1.…”

Section: Dihydroquinoline-3-carboxylic Acid 5a-fmentioning

confidence: 99%

“…[9][10][11][12] Chemical modifications at C3 and C7 of typical quinolone scaffold have the greatest influence on their activity [13], where position 7 largely affects activity, access and direction toward different molecular targets. [14][15][16][17][18] Moreover, introducing bulky groups at C7 was reported to broaden the spectrum of antibacterial activity and reduce the likelihood of developing resistance. [19][20][21] Currently, used quinolones drugs became also subjects for structural variation and derivatization.…”

Section: Introductionmentioning

confidence: 99%

Antibacterial and Urease Inhibitory activity of New Piperazinyl N-4 Functionalized Ciprofloxacin-oxadiazoles

Abdel-AAl

Abdel‐Aziz

Shaykoon

et al. 2019

Journal of Modern Research

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This research includes design of new ciprofloxacin bearing oxadiazole at the N-4 piperazinyl for the purpose of having urease inhibitory activity as well as antibacterial activity. Hence, a group of new N-4 piperazinyl oxdiazole derivatives of ciprofloxacin was prepared and characterized using different spectroscopic and analytical techniques including 1 H-NMR, 13 C-NMR, MS and elemental analysis. Compounds 5b and 5c experienced moderate activity against the urease producing Klebsiella pneumoniae strains better than the standard drug used chloramphenicol and less than the parent drug ciprofloxacin. On the other hand, most of the tested compounds showed a urease inhibitory activity more than the parent drug, ciprofloxacin and comparable to standard, thiourea. The docked compounds exhibited better binding to urease enzyme of H. pylori than standard, AHA with binding scores for correlate to the antiurease assay results. Compound 5b was the most potent anti-Klebsiella pneumoniae urease inhibitor with activity higher the standard (IC 50 = 67.8 and 78.89 µM, respectively).

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“…To evaluate DNA damage, comet assay was performed using single-cell gel electrophoresis with a Trevigen kit (Gaithersburg, MD) according to the method previously reported [41] Briefly, HCT15 cells, seeded in a density of 1 x 10 5 …”

Section: Comet Assaymentioning

confidence: 99%

Synthesis and biological activity of 2,4-di-p-phenolyl-6-2-furanyl-pyridine as a potent topoisomerase II poison

Karki

Park

Jun

et al. 2015

European Journal of Medicinal Chemistry

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Novel N-4-piperazinyl-ciprofloxacin-chalcone hybrids: Synthesis, physicochemical properties, anticancer and topoisomerase I and II inhibitory activity

Cited by 107 publications

References 33 publications

Modifications of quinolones and fluoroquinolones: hybrid compounds and dual-action molecules

Modifications of quinolones and fluoroquinolones: hybrid compounds and dual-action molecules

Antibacterial and Urease Inhibitory activity of New Piperazinyl N-4 Functionalized Ciprofloxacin-oxadiazoles

Synthesis and biological activity of 2,4-di-p-phenolyl-6-2-furanyl-pyridine as a potent topoisomerase II poison

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