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Synthesis of a new class of pyrrolo[3,4-h]quinazolines with antimitotic activity

  • Authors: Spanò, V; Montalbano, A; Carbone, A; Parrino, B; Diana, P; Cirrincione, G; Castagliuolo, I; Brun, P; Issinger, O-G; Tisi, S; Primac, I; Vedaldi, D; Salvador, A; Barraja, P
  • Publication year: 2014
  • Type: Articolo in rivista (Articolo in rivista)
  • OA Link:


A new series of pyrrolo[3,4-h]quinazolines was conveniently prepared with a broad substitution pattern. A large number of derivatives was obtained and the cellular cytotoxicity was evaluated in vitro against 5 different human tumor cell lines with GI50 values reaching the low micromolar level (1.3e19.8 mM). These compounds were able to induce cell death mainly by apoptosis through a mitochondrial dependent pathway. Selected compounds showed antimitotic activity and a reduction of tubulin polymerization in a concentration-dependent manner. Moreover, they showed anti-angiogenic properties since reduced in vitro endothelial cell migration and disrupted HUVEC capillary-like tube network in Matrigel.