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 [1]. Currently, particular attention is focused on such a class of compounds due to the affinity with sigma receptor and their relationship with cancer [2].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 [3]. Synthesis and biological results will be presented. [1] G. Mariappan, B.P. Saha, L. Sutharson, Anki, S. Garg, L. Pandey, D. Kumar, J. Pharm. Res., 2010, 3(12), 2856. [2] E. Aydar, C.P. Palmer, M. B. A. Djamoz, Cancer Res., 2004, 64, 5029. [3] A.M., Almerico, F. Mingoia, P. Diana, P. Barraja, A. Lauria, A. Montalbano, G Cirrincione, G. Dattolo, J. Med. Chem., 2005, 48, 2859.

Mingoia, F., Muriana, R., Fazzari, M., Alfio, A., Di Sano, C., Martorana, A., et al. (2011). Synthesis and antiproliferative activity of Naphtalenyl substituted 1,2-dihydropyrazol-5-one and related fused tetrazine. In XXIV Congresso Nazionale della Società Chimica Italina (pp.428). Lecce.

Synthesis and antiproliferative activity of Naphtalenyl substituted 1,2-dihydropyrazol-5-one and related fused tetrazine

MURIANA, Rosaria;FAZZARI, Marco;ALFIO, Alessia;MARTORANA, Annamaria;ALMERICO, Anna Maria;LAURIA, Antonino
2011-01-01

Abstract

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 [1]. Currently, particular attention is focused on such a class of compounds due to the affinity with sigma receptor and their relationship with cancer [2].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 [3]. Synthesis and biological results will be presented. [1] G. Mariappan, B.P. Saha, L. Sutharson, Anki, S. Garg, L. Pandey, D. Kumar, J. Pharm. Res., 2010, 3(12), 2856. [2] E. Aydar, C.P. Palmer, M. B. A. Djamoz, Cancer Res., 2004, 64, 5029. [3] A.M., Almerico, F. Mingoia, P. Diana, P. Barraja, A. Lauria, A. Montalbano, G Cirrincione, G. Dattolo, J. Med. Chem., 2005, 48, 2859.
Settore CHIM/08 - Chimica Farmaceutica
Settore CHIM/06 - Chimica Organica
set-2011
XXIV Congresso Nazionale della Società Chimica Italina
Lecce
11-16 settembre 2011
1
Mingoia, F., Muriana, R., Fazzari, M., Alfio, A., Di Sano, C., Martorana, A., et al. (2011). Synthesis and antiproliferative activity of Naphtalenyl substituted 1,2-dihydropyrazol-5-one and related fused tetrazine. In XXIV Congresso Nazionale della Società Chimica Italina (pp.428). Lecce.
Proceedings (atti dei congressi)
Mingoia, F; Muriana, R; Fazzari, M; Alfio, A; Di Sano, C; Martorana, A; Almerico, AM; Lauria, A
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/97106
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