In vitro cytotoxicity screening of some 3-substituted-4-oxo-imidazolidin-2-(1H)-thione derivatives as anticancer drug

Abstract

Aim: This study aimed to investigate the in vitro antitumor activity of new series of 2-thiohydanotin derivatives (7 and 9) against two cancer cell lines. Materials & methods: A new series of 2-thioxoimidazolidine derivatives (3–9) were synthesized and investigated for its structure through spectral analysis and also tested against (HepG-2) and (HCT-116) cell line. Results: Among the synthesized compounds, compound 7 halted liver cancer cells at the G0/G1 phase and triggered apoptosis of liver cancer. Contrarily, compound 9 caused colon cancer cells to be arrested at the S phase and trigger apoptosis. Also, they had a good inhibitory effect on (Nrf2). Conclusion: Both compounds had attractive lead molecules for the creation of colon and liver cancer medications.

Summary points

• A series of 3-substituted-4-oxo-imidazolidin-2-(1H)-Thione derivatives (3–9) were synthesized and assessed for their anticancer effect on HepG-2 and HCT-116.

• The chemical composition of the produced chemicals was verified using methods of elemental analysis and spectroscopy, such as ¹H, ¹³C NMR, MS and IR.

• Cytotoxicity screening found both compounds (7 and 9) had a good antiproliferation activity against HepG-2 and HCT-116 cancer cell lines.

• The outcomes of the cell cycle analysis showed that the most active compound 9 arrests colon cancer cells at the S phase, induces the apoptosis of colon cancer cells, and exhibits a good inhibitory effect against Nrf2.

• Compound 7 arrests liver cancer cells at the G0/G1 phase, induces apoptosis in liver cancer, and exhibits a great inhibitory effect against Nrf2.

• According to these findings, the newly discovered 2-thioxoimidazolin-4-one family offers a good framework for discovering more potential anticancer drugs.

Keywords: :

• 2-thioxoimidazolidine derivatives
• antiproliferation
• cell cycle arrest
• colon cancer
• liver cancer
• NF-E2-related factor
• Nrf2
• quantitative real time PCR

Supplemental material

Supplementary data for this article can be accessed at https://doi.org/10.1080/17568919.2024.2350925

Financial disclosure

The authors have no financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Competing interests disclosure

The authors have no competing interests or relevant affiliations with any organization or entity with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Writing disclosure

No writing assistance was utilized in the production of this manuscript.

Data availability statements

Samples of the synthesized compounds, HepG-2 and HCT-116 cell line are available from the authors.