Synthesis and antiproliferative activity of Naphtalenyl substituted 1,2-dihydropyrazol-5-one and related fused tetrazine
- Autori: Mingoia, F; Muriana, R; Fazzari, M; Alfio, A; Di Sano, C; Martorana, A; Almerico, AM; Lauria, A
- Anno di pubblicazione: 2011
- Tipologia: eedings
- Parole Chiave: antiproliferative activity, 1,1-dihydropyrazol-5-one, tetrazinone,
- OA Link: http://hdl.handle.net/10447/97106
In recent years, besides the main field of nonsteroidal anti-inflammatory agents, the interest towards pyrazolone derivatives has been renewed because of their wide biological and pharmacological applications . Currently, particular attention is focused on such a class of compounds due to the affinity with sigma receptor and their relationship with cancer .To these purposes we planned to design, synthesize and evaluate the antiproliferative activity (MTS assays) of a new series of 3-methyl-2-(1-R-naphthalen-2-yl)-1,2-dihydropyrazol-3-one derivatives 1 against HeLa, MCF-7, LAN-5, Caco2 in order to explore their anticancer potential. Additionally, further elaboration of the amino derivative 1 led to the tetracycle 2, possessing a reactive tetrazinone core which conferred valuable antiproliferative activity as previously reported . Synthesis and biological results will be presented.  G. Mariappan, B.P. Saha, L. Sutharson, Anki, S. Garg, L. Pandey, D. Kumar, J. Pharm. Res., 2010, 3(12), 2856.  E. Aydar, C.P. Palmer, M. B. A. Djamoz, Cancer Res., 2004, 64, 5029.  A.M., Almerico, F. Mingoia, P. Diana, P. Barraja, A. Lauria, A. Montalbano, G Cirrincione, G. Dattolo, J. Med. Chem., 2005, 48, 2859.