From Infection to Tumor: Exploring the Therapeutic Potential of Ciprofloxacin Derivatives as Anticancer Agents

Pharmaceuticals, Год журнала: 2025, Номер 18(1), С. 72 - 72

Опубликована: Янв. 9, 2025

Ciprofloxacin, a widely used second-generation fluoroquinolone for treating bacterial infections, has recently shown notable anticancer properties. This review explores progress in developing ciprofloxacin derivatives with properties, emphasizing key structural changes that improve their therapeutic effectiveness by modifying the basic group at position 7, carboxylic acid 3, or both. It further investigates mechanisms which these fight cancer, such as inducing apoptosis, arresting cell cycle, inhibiting topoisomerase I and II, preventing tubulin polymerization, suppressing interleukin 6, blocking thymidine phosphorylase, multidrug resistance proteins, hindering angiogenesis. Additionally, it outlines future directions, enhancing efficacy, selectivity, investigating potential synergy other chemotherapeutic agents, offering promising avenue new therapies cancer.

Язык: Английский

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Design, Synthesis, Anticancer Screening, and Mechanistic Study of Spiro-N-(4-sulfamoyl-phenyl)-1,3,4-thiadiazole-2-carboxamide Derivatives

International Journal of Molecular Sciences, Год журнала: 2025, Номер 26(2), С. 863 - 863

Опубликована: Янв. 20, 2025

The present study aims to create spiro-N-(4-sulfamoyl-phenyl)-1,3,4-thiadiazole-2-carboxamide derivatives with anticancer activities. in vitro evaluation showed that only the novel spiro-acenaphthylene tethered-[1,3,4]-thiadiazole (compound 1) exhibited significant efficacy as a selective inhibitor of tumor-associated isoforms carbonic anhydrase. Compound 1 demonstrated considerable against renal RXF393, colon HT29, and melanoma LOX IMVI cancer cell lines, IC50 values 7.01 ± 0.39, 24.3 1.29, 9.55 0.51 µM, respectively. In comparison, doxorubicin 13.54 0.82, 13.50 0.71, 6.08 0.32 µM for corresponding lines. Importantly, compound lower toxicity normal WI 38 line than doxorubicin, 46.20 2.59 18.13 0.93 respectively, indicating greater selectivity target compared standard agent doxorubicin. Also, mechanistic experiments exhibits inhibitory activity human anhydrase hCA IX XII, 0.477 0.03 1.933 0.11 μM, enhanced cancer-associated over cytosolic I II, 7.353 0.36 12.560 0.74 Cell cycle studies revealed caused G1 phase arrest RXF393 cells, apoptosis verified substantial induction levels early late apoptosis, well necrosis (11.69%, 19.78%, 3.66%, respectively), comparable those induced by conventional cytotoxic at 9.91%, 23.37%, 6.16%, Molecular docking confirmed strong binding affinity active sites highlighting interactions zinc-binding groups hydrophobic residues. These findings underscore compound’s potential viable via targeting CA.

Язык: Английский

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Repurposing antibiotics: A dual-action approach against bacteria-induced cancer

Cancer Pathogenesis and Therapy, Год журнала: 2025, Номер unknown

Опубликована: Фев. 1, 2025

Язык: Английский

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Discovery of a novel 4-pyridyl SLC-0111 analog targeting tumor-associated carbonic anhydrase isoform IX through tail-based design approach with potent anticancer activity

Frontiers in Chemistry, Год журнала: 2025, Номер 13

Опубликована: Апрель 4, 2025

Introduction: Carbonic anhydrase IX (CA IX) is a tumor-associated enzyme involved in cancer progression and survival. Targeting CA with selective inhibitors like SLC-0111 has shown therapeutic potential. This study aimed to develop novel 4-pyridyl analog ( Pyr ) of enhanced anticancer activity. Methods: was synthesized using tail-based design characterized by NMR. Its cytotoxicity tested against normal cell lines. inhibition, cycle effects, apoptosis induction, protein expression changes were evaluated. Molecular docking ADMET predictions assessed binding drug-like properties. Results Discussion: showed toward cells potent inhibition. It induced G0/G1 arrest, apoptosis, modulated p53, Bax, Bcl-2 levels. Docking confirmed strong binding, analysis indicated good oral bioavailability. These results support as promising candidate.

Язык: Английский

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Design, Synthesis, and In Silico Studies of New Norfloxacin Analogues with Broad Spectrum Antibacterial Activity via Topoisomerase II Inhibition

Pharmaceuticals, Год журнала: 2025, Номер 18(4), С. 545 - 545

Опубликована: Апрель 8, 2025

Background: Novel norfloxacin derivatives were synthesized, characterized, and screened for their antibacterial activity against Gram-positive strain S. aureus ATCC 6538 Gram-negative strains; E. coli 25923, K. pneumoniae 10031, P. aeruginosa 27853 using the agar cup diffusion method. Results: The results revealed that compounds 6–17 exhibited more potent towards with MIC values of 0.21–3.61 µM than a 7.83 µM. most compound, 6, showed 37-fold potency norfloxacin. More importantly, compound 7 MRSA norfloxacin, 0.80 1.96 µM, respectively. Meanwhile, 15 16 have strains 0.20–0.79 compared 0.24 Moreover, higher topoisomerase II enzymes, especially IV, which confirms docking study gyrase enzyme active binding site (PDB ID: 2XCT). In addition, cytotoxicity assays 7, 15, negligible risks toxic effects when evaluated normal cell line WI 38. Conclusions: on (PDB: 2XCT) aligns inhibition. physicochemical pharmacokinetic characteristics target forecasted via SwissADME. Hence, these are considered promising candidates require further optimization.

Язык: Английский

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Unveiling the therapeutic potential of 1,2,4-oxadiazole derivatives: An updated review

Results in Chemistry, Год журнала: 2025, Номер unknown, С. 102271 - 102271

Опубликована: Апрель 1, 2025

Язык: Английский

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Synergistic Potential of Antibiotics with Cancer Treatments

Cancers, Год журнала: 2024, Номер 17(1), С. 59 - 59

Опубликована: Дек. 28, 2024

Intratumoral microbiota, the diverse community of microorganisms residing within tumor tissues, represent an emerging and intriguing field in cancer biology. These microbial populations are distinct from well-studied gut offering novel insights into biology, progression, potential therapeutic interventions. Recent studies have explored use certain antibiotics to modulate intratumoral microbiota enhance efficacy therapies, showing promising results. Antibiotics can alter microbiota’s composition, which may a major role promoting progression immune evasion. Certain bacteria tumors promote immunosuppression resistance therapies. By targeting these bacteria, help create more favorable environment for chemotherapy, targeted therapy, immunotherapy act effectively. Some microenvironment produce immunosuppressive molecules that inhibit activity cells. The combination other therapies holds significant promise creating synergistic effect enhancing response against cancer. In this review, we analyze several preclinical been conducted demonstrate synergy between discuss possible clinical implications.

Язык: Английский

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