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Your search keyword '"Cisplatin and cancer"' showing total 2 results
Start Over Descriptor "Cisplatin and cancer" Topic fluoroquinolones
2 results on '"Cisplatin and cancer"'

1. A Novel Class of Functionalized Synthetic Fluoroquinolones with Dual Antiproliferative - Antimicrobial Capacities.

Author

Al-Nuaimi A, Al-Hiari Y, Kasabri V, Haddadin R, Mamdooh N, Alalawi S, and Khaleel S

Subjects
Anti-Infective Agents chemical synthesis, Antineoplastic Agents chemical synthesis, Candida albicans drug effects, Cell Line, Tumor, Cell Survival drug effects, Drug Design, Escherichia coli drug effects, Fluoroquinolones chemical synthesis, Humans, Microbial Sensitivity Tests, Staphylococcus aureus drug effects, Anti-Infective Agents pharmacology, Antineoplastic Agents pharmacology, Cell Proliferation drug effects, Fluoroquinolones pharmacology
Abstract

As vosaroxin as a fluoroquinolone (FQ) had anticancer effectiveness; this study aimed to screen new lipophilic FQs for their dual antimicrobial-antiproliferative activities. Using sulforhodamine B assay; 36 lipophilic FQs have been screened for antimicrobial propensities against S. aureus, E. coli, and C. albicans vs. the respective references ciprofloxacin and fluconazole. They were also explored against a battery of cancer cell lines. Normal periodontal ligament fibroblasts (PDL) were tested for safety examination in comparison to the cisplatin. Reduced FQ compound 4g (R-2, 4-DMeOACA) highly scored nanomolar potency with MIC value of 0.004 µM against gram-positive bacteria. The highest activity of the 36 lipophilic FQs was noted on Leukaemia K562, cervical HELA and pancreatic PANC-1 cancer cell lines with respective IC50 value of 0.005 µM for compound R-4-BuACA (4e), 0.40 µM with CHxCA (7a) and 0.11 µM for R-4-HxACA (4f). Tested FQs exhibited cytotoxicity in A549 lung cancer, MCF-7 and T47D breast cancer cell lines. The reduced 4e and 4f compounds have shown nanomolar inhibition against K562 (as of 4e), PANC-1 and MCF-7 (as of 4f) with IC50 values of 0.005, 0.11 and 0.30 µM, respectively. Succinctly FQs' dual gram-positive antibacterial-antineoplastic capacities expand on of drug design scaffolds in lead generation., .

Published
2021
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2. A Novel Class of Functionalized Synthetic Fluoroquinolones with Dual Antiproliferative - Antimicrobial Capacities

Author

Violet Kasabri, Randa N. Haddadin, Sundus Alalawi, Noor Mamdooh, Abdelrahman Al-Nuaimi, Sara Khaleel, and Yusuf Al-Hiari

Subjects
0301 basic medicine, Staphylococcus aureus, Cell Survival, Sulforhodamine B, Antineoplastic Agents, Microbial Sensitivity Tests, Quinolones, Cisplatin and cancer, Pharmacology, Vosaroxin, HeLa, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Anti-Infective Agents, Cell Line, Tumor, Candida albicans, Escherichia coli, medicine, Humans, Potency, Cytotoxicity, IC50, Cell Proliferation, biology, General Medicine, Antimicrobial, biology.organism_classification, Ciprofloxacin, 030104 developmental biology, chemistry, Drug Design, 030220 oncology & carcinogenesis, Triazoloquinolones, Sulphorodhamine B, Research Article, Fluoroquinolones, medicine.drug
Abstract

As vosaroxin as a fluoroquinolone (FQ) had anticancer effectiveness; this study aimed to screen new lipophilic FQs for their dual antimicrobial-antiproliferative activities. Using sulforhodamine B assay; 36 lipophilic FQs have been screened for antimicrobial propensities against S. aureus, E. coli, and C. albicans vs. the respective references ciprofloxacin and fluconazole. They were also explored against a battery of cancer cell lines. Normal periodontal ligament fibroblasts (PDL) were tested for safety examination in comparison to the cisplatin. Reduced FQ compound 4g (R-2, 4-DMeOACA) highly scored nanomolar potency with MIC value of 0.004 µM against gram-positive bacteria. The highest activity of the 36 lipophilic FQs was noted on Leukaemia K562, cervical HELA and pancreatic PANC-1 cancer cell lines with respective IC50 value of 0.005 µM for compound R-4-BuACA (4e), 0.40 µM with CHxCA (7a) and 0.11 µM for R-4-HxACA (4f). Tested FQs exhibited cytotoxicity in A549 lung cancer, MCF-7 and T47D breast cancer cell lines. The reduced 4e and 4f compounds have shown nanomolar inhibition against K562 (as of 4e), PANC-1 and MCF-7 (as of 4f) with IC50 values of 0.005, 0.11 and 0.30 µM, respectively. Succinctly FQs' dual gram-positive antibacterial-antineoplastic capacities expand on of drug design scaffolds in lead generation.br /.

Published
2021
Full Text
View/download PDF

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