Abstract
A natural like O-glycoconjugate polycyclic compound 4 was obtained by a multistep procedure starting from N-(3-methyl-1-(4-nitrophenyl)-1H-pyrazol-5-yl)acetamide. The glycosyl derivative 4 showed antiproliferative activity against all the tumoral cell lines of the NCI panel in the range 0.47–5.43 μM. Cytofluorimetric analysis performed on MDA-MB231, a very aggressive breast cancer cell line, which does not express estrogen, progesterone and HER-2/neu receptors, showed that 4 is able to induce prolonged cell cycle arrest at G2/M phase and morphological signs of differentiation. These events are correlated with down-regulation of both cyclin B1 and cdc2, the cyclins involved in G2/M transition, as well as up-regulation of cyclin-dependent kinase (CDK) inhibitor p21 Cip1/Waf1.
| Lingua originale | English |
|---|---|
| pagine (da-a) | 247-256 |
| Numero di pagine | 10 |
| Rivista | European Journal of Medicinal Chemistry |
| Volume | 122 |
| Stato di pubblicazione | Published - 2016 |
All Science Journal Classification (ASJC) codes
- Pharmacology
- Drug Discovery
- Organic Chemistry
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Plescia, F., Daidone, G., Raimondi, M. V., Raffa, D., Lauricella, M., D'Anneo, A., Maggio, B., Prosa, N., & Scherrmann, M-C. (2016). Synthesis and antiproliferative activity of a natural like glycoconjugate polycyclic compound. European Journal of Medicinal Chemistry, 122, 247-256.