New 1,2,3-triazole linked ciprofloxacin-chalcones induce DNA damage by inhibiting human topoisomerase I&amp; II and tubulin polymerization

Mohammed, Hamada H.H.; El-Hafeez, Amer Ali Abd; Ebeid, Kareem; Mekkawy, Aml I; Abourehab, Mohammed A.S.; Wafa, Emad I.; Alhaj‐Suliman, Suhaila O.; Salem, Aliasger K.; Ghosh, Pradipta; Abuo‐Rahma, Gamal El‐Din A.; Hayallah, Alaa M.; Abbas, Samar H.

doi:10.1080/14756366.2022.2072308

Cited by 33 publications

(17 citation statements)

References 80 publications

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“…It is well known that the CPX, as all FQs, are a bacterial topoisomerase inhibitor [6,69]. However, due to the presence of these enzymes in the human body, in the last years many experimental researches have been pointed the potential of this drug and its derivatives to also inhibit human topoisomerases [12,[70][71][72][73][74][75][76]. Recently, in order to better understand the action mechanisms and the main differences between the interactions in TOPO-II of the two organisms, some theoretical investigations have already been done [77,78].…”

Section: Resultsmentioning

confidence: 99%

Structural parameters of the interaction between ciprofloxacin and human topoisomerase-II β enzyme: toward new 19F NMR Chemical Shift probes

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Ramalho

Gonçalves

2022

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New tools for cancer diagnosis are being studied day by day, since early diagnosis can be crucial for a successful treatment. In this context, the use of NMR probes constitutes an efficient way of diagnosis. In this work, we investigated the use of ciprofloxacin to indirectly label the overexpression of topoisomerase-II enzymes by changes in 19F NMR chemical shifts of ciprofloxacin. Increased topoisomerase-II expression has been associated with cancer occurrence, mainly with aggressive forms of breast cancer, thus constituting a promising molecular target for new tumor cell identifiers. Using DFT calculations, a spectroscopy analysis of ciprofloxacin in different chemical environments, evaluating the solvent and enzymatic effects was performed. Our results point that the ciprofloxacin forms a stable complex with the enzyme, and the main intermolecular interactions between ciprofloxacin and human topoisomerase-IIβ are hydrogen bonds, following by pi-pi stacking and electrostatic interactions. Also, a shift of 6.04 ppm occurs in the 19F NMR signal when ciprofloxacin is interacting with the human topoi-somerase-IIβ enzyme, and that this parameter may be a possible indirect marker to indicate the overexpression of these enzymes in the body.

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Section: Resultsmentioning

confidence: 99%

Structural parameters of the interaction between ciprofloxacin and human topoisomerase-II β enzyme: toward new 19F NMR Chemical Shift probes

Sales

Ramalho

Gonçalves

2022

Preprint

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“…Copper-catalyzed 1,3-dipolar cycloaddition (CuAAC) to form 1,2,3-triazoles is the most popular reaction in click chemistry. Recently, 1,2,3-triazole backbones with hydrogen bonds, moderate dipole moments and enhanced water solubility had been widely used to generate drug candidates of anti-tumor ( Brown et al, 2022 ; Elganzory et al, 2022 ; Mohammed et al, 2022 ; Oekchuae et al, 2022 ; Oliveira et al, 2022 ; Mironov et al, 2023 ), anti-seizure ( Bhattacherjee et al, 2022 ), anti-diabetic ( Dhameja et al, 2022 ), anti-parasitic ( Aljohani et al, 2022 ), anti-bacterial ( Daher et al, 2022 ; Mokariya et al, 2022 ; Nsira et al, 2022 ) and anti-viral ( Kutkat et al, 2022 ; Tatarinov et al, 2022 ) via CuAAC click chemistry ( Figure 1A ).…”

Section: Click Chemistrymentioning

confidence: 99%

Recent updates in click and computational chemistry for drug discovery and development

et al. 2023

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Drug discovery is a costly and time-consuming process with a very high failure rate. Recently, click chemistry and computer-aided drug design (CADD) represent popular areas for new drug development. Herein, we summarized the recent updates in click and computational chemistry for drug discovery and development including clicking to effectively synthesize druggable candidates, synthesis and modification of natural products, targeted delivery systems, and computer-aided drug discovery for target identification, seeking out and optimizing lead compounds, ADMET prediction as well as compounds synthesis, hopefully, inspires new ideas for novel drug development in the future.

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“…Plates were then incubated at 37°C with 5% CO 2 for 48 hours. Next, Cell Titer 96 aqueous MTS reagent [3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide, purchased from Promega Corporation, San Luis Obispo, CA] was added to the cells following the manufacturer's instructions (63,(68)(69)(70). After incubation for 2 hours, cell viability (%) was calculated on the basis of the absorbance measured at 490 nm using a SpectraMax Plus spectrophotometer (Molecular Devices, San Jose, CA).…”

Section: Cytotoxicity Studymentioning

confidence: 99%

Cationic nanoparticles enhance T cell tumor infiltration and antitumor immune responses to a melanoma vaccine

et al. 2022

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In clinical settings, cancer vaccines as monotherapies have displayed limited success compared to other cancer immunotherapeutic treatments. Nanoscale formulations have the ability to increase the efficacy of cancer vaccines by combatting the immunosuppressive nature of the tumor microenvironment. Here, we have synthesized a previously unexplored cationic polymeric nanoparticle formulation using polyamidoamine dendrimers and poly( d , l -lactic- co -glycolic acid) that demonstrate adjuvant properties in vivo. Tumor-challenged mice vaccinated with an adenovirus-based cancer vaccine [encoding tumor-associated antigen (TAA)] and subsequently treated with this nanoparticulate formulation showed significant increases in TAA-specific T cells in the peripheral blood, reduced tumor burden, protection against tumor rechallenge, and a significant increase in median survival. An investigation into cell-based pathways suggests that administration of the nanoformulation at the site of the developing tumor may have created an inflammatory environment that attracted activated TAA-specific CD8 + T cells to the vicinity of the tumor, thus enhancing the efficacy of the vaccine.

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New 1,2,3-triazole linked ciprofloxacin-chalcones induce DNA damage by inhibiting human topoisomerase I& II and tubulin polymerization

Cited by 33 publications

References 80 publications

Structural parameters of the interaction between ciprofloxacin and human topoisomerase-II β enzyme: toward new 19F NMR Chemical Shift probes

Structural parameters of the interaction between ciprofloxacin and human topoisomerase-II β enzyme: toward new 19F NMR Chemical Shift probes

Recent updates in click and computational chemistry for drug discovery and development

Cationic nanoparticles enhance T cell tumor infiltration and antitumor immune responses to a melanoma vaccine

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