Novel Polycarbo-Substituted Imidazo[1,2-c] quinazolines: Synthesis and Cytotoxicity Study

作者：Khoza Tebogo Ankie; Makhafola Tshepiso Jan; Mphahlele Malose Jack^*

来源：Molecules, 2015, 20(12): 22520-22533.

DOI：10.3390/molecules201219863

• dihalogenated 2H-imidazo[1,2-c]quinazolines
• cross-coupling
• imidazo[1,2-c]quinazolines
• cytotoxicity

Amination of the 2-aryl-6-bromo-4-chloro-8-iodoquinazolines with 2-aminoethanol followed by acid-promoted cyclodehydration of the incipient 2-((6,8-dihalo-2-phenylquinazolin-4-yl)amino)ethanols afforded the corresponding novel 5-aryl-9-bromo-7-iodo-2,3-dihydro-2H-imidazo[1,2-c]quinazolines. The latter were, in turn, subjected to sequential (Sonogashira and Suzuki-Miyaura) and one-pot two-step (Sonogashira/Stille) cross-coupling reactions to afford diversely functionalized polycarbo-substituted 2H-imidazo[1,2-c]quinazolines. The imidazoquinazolines were screened for in vitro cytotoxicity against human breast adenocarcinoma (MCF-7) cells and human cervical cancer (HeLa) cells.

• 出版日期2015-12