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

Barbara Parrino, Anna Carbone, Paola Barraja, Girolamo Cirrincione, Virginia Spano', Patrizia Diana, Alessandra Montalbano, Alessia Salvador, Silvia Tisi, Irina Primac, Irina Primac, Paola Brun, Paola Brun, Ignazio Castagliuolo, Daniela Vedaldi, Olaf-Georg Issinger

Risultato della ricerca: Articlepeer review

42 Citazioni (Scopus)

Abstract

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 5different 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 dependentpathway. Selected compounds showed antimitotic activity and a reduction of tubulin polymerizationin a concentration-dependent manner. Moreover, they showed anti-angiogenic properties sincereduced in vitro endothelial cell migration and disrupted HUVEC capillary-like tube network in Matrigel.
Lingua originaleEnglish
pagine (da-a)340-357
Numero di pagine18
RivistaEuropean Journal of Medicinal Chemistry
Volume74
Stato di pubblicazionePublished - 2014

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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