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A Novel Class of Functionalized Synthetic Fluoroquinolones with Dual Antiproliferative - Antimicrobial Capacities
- Source :
- Asian Pacific Journal of Cancer Prevention : APJCP
- Publication Year :
- 2021
- Publisher :
- EpiSmart Science Vector Ltd, 2021.
-
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 /.
- 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
Subjects
Details
- ISSN :
- 2476762X
- Volume :
- 22
- Database :
- OpenAIRE
- Journal :
- Asian Pacific Journal of Cancer Prevention
- Accession number :
- edsair.doi.dedup.....05a9e8ea53e510d30115f67d8c2cbba9
- Full Text :
- https://doi.org/10.31557/apjcp.2021.22.4.1075