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

par 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
Référence European journal of medicinal chemistry, 74, page (340-357)
Publication Publié, 2014-03

Article révisé par les pairs

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Résumé :

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.