1148040-91-8Relevant articles and documents
Synthesis of a new class of pyrrolo[3,4-h]quinazolines with antimitotic activity
Spanò, Virginia,Montalbano, Alessandra,Carbone, Anna,Parrino, Barbara,Diana, Patrizia,Cirrincione, Girolamo,Castagliuolo, Ignazio,Brun, Paola,Issinger, Olaf-Georg,Tisi, Silvia,Primac, Irina,Vedaldi, Daniela,Salvador, Alessia,Barraja, Paola
supporting information, p. 340 - 357 (2014/02/14)
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 (1.3-19.8 μM). 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.