Synthesis and evaluation of cytotoxicity of 6-amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitriles
| Autor: | Ali Shiri, Mehdi Bakavoli, Abdolhossien Massoudi, Hoda Atapour-Mashhad, Mohammad Soukhtanloo |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
medicine.diagnostic_test
010405 organic chemistry Organic Chemistry General Medicine Biology 01 natural sciences Biochemistry Molecular biology 0104 chemical sciences Flow cytometry 03 medical and health sciences chemistry.chemical_compound HT29 Cells 0302 clinical medicine chemistry Cell culture 030220 oncology & carcinogenesis medicine DNA fragmentation MTT assay DAPI Propidium iodide Viability assay |
| Zdroj: | Russian Journal of Bioorganic Chemistry. 42:316-322 |
| ISSN: | 1608-330X 1068-1620 |
| DOI: | 10.1134/s1068162016020047 |
| Popis: | Several derivatives of 6-amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitriles were synthesized via Biginelli type reaction and tested for their anti-proliferative activity on human breast cancer (MCF-7) and human colon carcinoma (HT29) cell lines. Malignant and non-malignant cells were cultivated in RPMI medium and incubated with different concentrations of these pyrimidines. Cell viability was evaluated by MTT assay. Apoptotic cells were determined using DAPI (4'-6-diamidino-2-phenylindole) and propidium iodide staining of DNA fragmentation by flow cytometry (sub-G1 peak). 6-Amino-4-(4-chlorophenyl)-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile and 6-amino-4-[4-dimethylamino)phenyl]-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile decreased the viability of MCF-7 and HT29 cells, in contrast to L929 cells. These compounds induced a sub-G1 peak inflow cytometry histograms of treated cells indicating that apoptosis is involved in their toxicity. |
| Databáze: | OpenAIRE |
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