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Evaluation of Anticancer Activity of Novel Sulfanyl-Substituted Hydrazone Compounds in Hepatocellular Carcinoma: In
Hatice Başpinar Küçük1, Tülay Yildiz1, Yaren Arasan2
1Faculty of Engineering, Department of Chemistry, Organic Chemistry Division, Istanbul University-Cerrahpasa, Istanbul 34320, Turkey.
Abstract:
Hepatocellular carcinoma is one of the hardest-to-treat cancer types, although some recent developments have been made. Therefore, the discovery of new treatment options is still desperately desired. In this study, some novel sulfanyl-substituted hydrazone compounds 2a-2h were synthesized and characterized using spectroscopic techniques (1H NMR, 13C NMR, IR, and HRMS). Then, hydrazone compounds were tested on four different cancer types (lung, hepatocellular, breast, and colon carcinoma) and one nonmalignant cell line. Among these hydrazone compounds and tested cancer types, compound 2c resulted in a satisfactory antigrowth effect against hepatocellular carcinoma, the HepG2 cell line. Further, in ovo antitumor and antiangiogenic assays were also performed together with the in silico calculations employed by target predictions of compound 2c by a tool called Way2Drug and then followed by binding affinity calculations to those targets by AutoDock Vina. The range of binding scores of compound 2c was calculated between -4 and -8.6 kcal/mol for those targets that were suggested to be involved in a local protein-protein interaction clustering on base excision repair and DNA topological change. It has been found that compound 2c might deserve further attention (e.g., animal studies for proof-of-concept) as a novel anticancer compound for the treatment of liver cancer.
Insights
Novel hydrazone compounds were synthesized and tested against cancer cells. Compound 2c showed significant anti-growth effects on liver cancer (hepatocellular carcinoma) cells, warranting further investigation as a potential new liver cancer treatment.
Area of Science:
- Medicinal Chemistry
- Oncology
- Molecular Biology
Background:
- Hepatocellular carcinoma (HCC) remains a challenging cancer to treat, necessitating the development of novel therapeutic strategies.
- Existing treatments for liver cancer have limitations, driving the search for new anticancer agents.
Purpose of the Study:
- To synthesize and characterize novel sulfanyl-substituted hydrazone compounds.
- To evaluate the anticancer potential of these compounds against various cancer cell lines, with a focus on hepatocellular carcinoma.
- To investigate the molecular mechanisms and binding affinities of the most promising compound through in silico and in ovo assays.
Main Methods:
- Synthesis and spectroscopic characterization (1H NMR, 13C NMR, IR, HRMS) of sulfanyl-substituted hydrazone compounds (2a-2h).
- In vitro screening of compounds against lung, hepatocellular, breast, and colon carcinoma cell lines, and a nonmalignant cell line.
- In ovo antitumor and antiangiogenic assays, alongside in silico target prediction (Way2Drug) and binding affinity calculations (AutoDock Vina).
Main Results:
- Compound 2c demonstrated significant antigrowth activity against the HepG2 hepatocellular carcinoma cell line.
- In silico analysis predicted that compound 2c targets proteins involved in base excision repair and DNA topological changes.
- Binding affinity calculations for compound 2c ranged from -4 to -8.6 kcal/mol for predicted targets.
Conclusions:
- Compound 2c exhibits promising anticancer properties against hepatocellular carcinoma, particularly its anti-proliferative effects on HepG2 cells.
- The identified molecular targets suggest a mechanism involving DNA repair and topological regulation.
- Compound 2c warrants further investigation, including preclinical animal studies, as a potential novel therapeutic agent for liver cancer.
