International Journal of Pharmacology (IJP) is published by IMR Press from Volume 21 Issue 4 (2025). Previous articles were published by another publisher under the CC-BY licence, and they are hosted by IMR Press on imrpress.com as a courtesy and upon agreement.
Biological Evaluation of Some Imidazolidine-2,4-dione and 2-thioxoimidazolidin-4-one Derivatives as Anticoagulant Agents and Inhibition of MCF-7 Breast Cancer Cell Line
1 Department of Botany and Microbiology, Collage of Science, King Saud University, P.O. Box 2455, 11451 Riyadh, Kingdom of Saudi Arabia
2 National Institute of Oceanography and Fisheries, Al-Kanater Al-Khairya Fish Research Station, Egypt
3 PG and Research Department of Chemistry, Nehru Memorial College, Puthanampatti-621007, Tiruchirappalli, Tamil Nadu, South India
4 Department of Medical Laboratory Sciences, College of Medicine and Health Sciences, Arba Minch University, Arba Minch, Ethiopia
Abstract
In this study, to investigate the synthesis and characterization of some imidazolidine-2,4-dione,2-thioxoimidazolidin-4-one derivatives and synthesized compounds were evaluated for anticoagulant and anticancer activities. Compounds 2a-2h, 3a-3h, 4a-4h and 5a-5h were prepared by cyclization method. The synthesized compounds were confirmed by Fourier transform infrared spectroscopy (IR), proton nuclear magnetic resonance (1H-NMR), carbon nuclear magnetic resonance (13C-NMR), Mass Spectrometry (MS) and elemental analyses. The synthesized compounds were screened for MCF-7 breast cancer cell line and anti-coagulant activities. Anticoagulant activity was determined by Activated Partial Thromboplastin Time (APTT) and Prothrombin Time (PT) coagulation assays. Compound 3-(2,6-bis (4-methoxyphenyl)-1,3-dimethylpiperidin-4-ylideneamino)-2-thioxoimi dazolidin-4-one 5f (>1000 in APTT assays) was highly response in anticoagulant screening compared with the reference of heparin while the compound 3-{[-1,3-Dimethyl-2,6-di (4’-nitrophenyl) piperidin-4-ylidene]amino}imidazolidine-2,4-dione 3e (LD50: 20.4 μg mL–1 was highly active against MCF-7 breast cancer cell line compared with the reference. Therefore, the compounds 5f and 3e are novel and beneficial for the development of anticoagulant and anticancer agents.
Keywords
- Imidazolidin-2,4-dione
- 2-thioxoimidazolidin-4-one
- anticoagulant activity
- anticancer activity
- APTT assay