الفهرس 
Chapter (1): CancerOnly 14 pages are availabe for public view
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Abstract
Background: Acridine derivatives have garnered significant attention from
medicinal chemists due to their diverse range of biological activities,
encompassing antifungal, parasitic, antiviral, antibacterial, and anticancer
properties. Methods: In this study, eleven compounds were synthesized
according to a previously established protocol, and their impact on cell growth
inhibition, induction of apoptosis, and cell cycle distribution was assessed in
human hepatocellular carcinoma HepG2 cells and human colon cells HCT-116
and breast MF-7. Furthermore, their inhibitory effects on the enzymes
topoisomerase (Topo) I and II were investigated in vitro using commercially
available DNA kit followed by PCR and gel electrophoresis. Molecular docking
studies were conducted to confirm the binding mechanism of these compounds
to the enzyme’s active site. Results: Compound 8b demonstrated the highest
potency against Topo-I, with an IC50 value of 3.41 µg/ml, while compound 7c
displayed a significant inhibitory effect on Topo II, with an IC50 of 7.33 µ/ml,
outperforming both the other compounds and the control drug. The efficacy of
compounds 7c and 8b against topoisomerases was consistent with their potent
anti-proliferative properties, which involved the induction of apoptosis and a
reduction in the S phase of the cell cycle. Molecular docking analysis suggested
that these two compounds exerted their anti-proliferative and proapoptotic
effects primarily through their potent inhibitory action on Topo II, rather than
on Topo I.
Conclusion: Compounds 7c and 8b hold promise as potential anti-cancer drugs
due to their anti-proliferative and proapoptotic effects, which are mediated by
their action on the Topoisomerase enzyme, particularly Topo II.