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GIUSEPPE DAIDONE

SYNTHESIS AND IN VITRO ANTILEUKEMIC ACTIVITY OF NEW 4-TRIAZENOPYRAZOLE DERIVATIVES

  • Autori: Daidone, G.; Maggio, B.; Raffa, D.; Plescia, S.; Schillaci, D.; Raimondi, M.
  • Anno di pubblicazione: 2004
  • Tipologia: Articolo in rivista (Articolo in rivista)

Abstract

Several new 4-(3,3-dimethyltriazeno)-5-benzamidopyrazole derivatives were prepared by reacting 4-diazo-5-benzamidopyrazole derivatives with dimethylamine. The compounds were tested at 10 μM for their vitro antileukemic activity against K562 (Human chronic myelogenous leukemia) and Raji (human Burkitt limphoma ) cell lines. Dacarbazine and methotrexate were used for comparative purpose. The 3-methyl-4-(3,3-dimethyltriazeno)-5-(substituted benzamido)pyrazoles, bearing the pyrazole nucleus free at 1 position, resulted more active than the 1-(substituted phenyl)-3-methyl-4-(3,3-dimethyltriazeno)-5-benzamidopyrazoles. Dacarbazine at 10 μM showed no activity in the above tests. The observed difference among Dacarbazine and the active 4-triazenopyrazoles migth be explained admiting that these last compounds, differently by Dacarbazine, did not follow a mechanism of action based on the cytochrome P-450 induced demethylation. The most active compound 2d showed growth inhibition values of 97.8 and 99.4% against K562 and Raji cell lines respectively. Methotrexate inhibition values at 0.2 μM against the above cell lines were 86.7 and 75.1% respectively.

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