article · Journal of Enzyme Inhibition and Medicinal Chemistry
Spirooxindoles form a central structural component in various naturally occurring bioactive molecules and synthetic substances. A synthetic series of spirooxindoles, designated 6a to 6p, was evaluated to determine anticancer actions against HepG2 hepatocellular carcinoma and PC-3 prostate cancer cell lines. Among the tested molecules, spirooxindole 6a demonstrated notable anti-proliferative capabilities against both cell types, recording half-maximal inhibitory concentrations of 6.9 micromolar in liver cancer cells and 11.8 micromolar in prostate cancer cells. Further biological assessment of spirooxindole 6a in HepG2 cells revealed that it triggers programmed cell death. This pro-apoptotic response was confirmed through a marked elevation in the Bax to Bcl-2 ratio alongside increased expression levels of the caspase-3 enzyme, highlighting its mechanistic role in halting malignant cell growth.
Liver and prostate cancers remain significant global health challenges that require new therapeutic interventions. Investigating privileged chemical scaffolds such as spirooxindoles offers useful starting points for oncology drug discovery. Demonstrating that a synthetic derivative can suppress malignant cell proliferation and activate cellular self-destruction mechanisms provides essential foundational knowledge for future therapeutic design.
This work represents early-stage, laboratory-based discovery that could interest pharmaceutical developers and medicinal chemists designing small-molecule oncology candidates. The identified compound serves as a preliminary lead for treating hepatocellular carcinoma and prostate cancer. Because the evidence is limited to in vitro cell assays, the technology remains distant from real-world medical use and requires extensive chemical optimisation, safety profiling, and preclinical animal testing.
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In the current medical era, spirooxindole motif stands out as a privileged heterospirocyclic scaffold that represents the core for a wide range of bioactive naturally isolated products (such as Strychnofoline and spirotryprostatins A and B) and synthetic compounds. Interestingly, no much attention has been paid to develop spirooxindole derivatives with dual antioxidant and anticancer activities. In this context, a series of spirooxindoles 6a-p was examined for their anticancer effect towards HepG2 hepatocellular carcinoma and PC-3 prostate cancer cell lines. Spirooxindole 6a was found to be an efficient anti-proliferative agent towards both HepG2 and PC-3 cells (IC50 = 6.9 and 11.8 µM, respectively). Afterwards, spirooxindole 6a was assessed for its apoptosis induction potential in HepG2 cells, where its pro-apoptotic impact was approved via the significant elevation in the Bax/Bcl-2 ratio and the expression levels of caspase-3.
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DOI: 10.1080/14756366.2020.1743281
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