Synthesis and induction of G0–G1 phase arrest with apoptosis of 3, 5-dimethyl-6-phenyl-8-(trifluoromethyl)-5, 6-dihydropyrazolo [3, 4-f][1, 2, 3, 5] tetrazepin-4 (3H)-one

…, F Plescia, M Tolomeo, E Barbusca, G Cannizzo…

Index: Maggio, Benedetta; Raffa, Demetrio; Raimondi, Maria Valeria; Cascioferro, Stella; Plescia, Fabiana; Tolomeo, Manlio; Barbusca, Eleonora; Cannizzo, Giuliana; Mancuso, Salvatrice; Daidone, Giuseppe European Journal of Medicinal Chemistry, 2008 , vol. 43, # 11 p. 2386 - 2394

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Citation Number: 9

Abstract

The multistep synthesis of 3, 5-dimethyl-6-phenyl-8-(trifluoromethyl)-5, 6-dihydropyrazolo [3, 4-f][1, 2, 3, 5] tetrazepin-4 (3H)-one 15 has been carried out. The compound showed antiproliferative and apoptotic effects against K562, K562-R (imatinib mesilate resistant), HL60 and multidrug resistant (MDR) HL60 cell lines. Compound 15 showed a pro-apoptotic activity against HL60 and K562 resistant cell lines markedly higher than etoposide and ...