Journal
INTERNATIONAL JOURNAL OF PHARMACOLOGY
Volume 12, Issue 4, Pages 290-303Publisher
ASIAN NETWORK SCIENTIFIC INFORMATION-ANSINET
DOI: 10.3923/ijp.2016.290.303
Keywords
Imidazolidin-2,4-dione; 2-thioxoimidazolidin-4-one; anticoagulant activity; anticancer activity; APTT assay
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Funding
- Deanship of Scientific Research at King Saud University [RGP-010]
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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 (H-1-NMR), carbon nuclear magnetic resonance (C-13-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-dione3e(LD50: 20.4 mu g 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.
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