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.
Al-Nuaimi, A., Al-Hiari, Y., Kasabri, V., Haddadin, R., Mamdooh, N., Alalawi, S., & Khaleel, S. (2021). A Novel Class of Functionalized Synthetic Fluoroquinolones with Dual Antiproliferative - Antimicrobial Capacities. Asian Pacific Journal of Cancer Prevention, 22(4), 1075-1086. doi: 10.31557/APJCP.2021.22.4.1075
MLA
Abdelrahman Al-Nuaimi; Yusuf Al-Hiari; Violet Kasabri; Randa Haddadin; Noor Mamdooh; Sundus Alalawi; Sara Khaleel. "A Novel Class of Functionalized Synthetic Fluoroquinolones with Dual Antiproliferative - Antimicrobial Capacities". Asian Pacific Journal of Cancer Prevention, 22, 4, 2021, 1075-1086. doi: 10.31557/APJCP.2021.22.4.1075
HARVARD
Al-Nuaimi, A., Al-Hiari, Y., Kasabri, V., Haddadin, R., Mamdooh, N., Alalawi, S., Khaleel, S. (2021). 'A Novel Class of Functionalized Synthetic Fluoroquinolones with Dual Antiproliferative - Antimicrobial Capacities', Asian Pacific Journal of Cancer Prevention, 22(4), pp. 1075-1086. doi: 10.31557/APJCP.2021.22.4.1075
VANCOUVER
Al-Nuaimi, A., Al-Hiari, Y., Kasabri, V., Haddadin, R., Mamdooh, N., Alalawi, S., Khaleel, S. A Novel Class of Functionalized Synthetic Fluoroquinolones with Dual Antiproliferative - Antimicrobial Capacities. Asian Pacific Journal of Cancer Prevention, 2021; 22(4): 1075-1086. doi: 10.31557/APJCP.2021.22.4.1075
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