1189363-90-3Relevant academic research and scientific papers
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
, 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.
Synthesis of the new ring system 6,8-dihydro-5H-pyrrolo[3,4-h]quinazoline
Barraja, Paola,Spanò, Virginia,Diana, Patrizia,Carbone, Anna,Cirrincione, Girolamo
scheme or table, p. 5389 - 5391 (2009/12/06)
A convenient synthesis of the pyrrolo[3,4-h]quinazoline ring system is reported. Our synthetic approach consisted of the annelation of a pyrimidine ring to an isoindole moiety using tetrahydroisoindole-4-ones as building blocks. The antiproliferative activity of the new compounds was investigated and one of them showed antitumor activity against all the 59 tested cell lines at micromolar concentrations (1.46-18.4 μM).
