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

  • Autori: Spano', V.; Montalbano, A.; Carbone, A.; Parrino, B.; Diana, P.; Cirrincione, G.; Castagliuolo, I.; Brun, P.; Issinger, O.; Tisi, S.; Primac, I.; Vedaldi, D.; Salvador, A.; Barraja, P.
  • Anno di pubblicazione: 2014
  • Tipologia: 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.