Title of article :
Synthesis and cytotoxic evaluation of novel quinozalinone derivatives with substituted benzimidazole in position 3
Author/Authors :
Taherian ، Elham - Isfahan University of Medical Sciences , Khodarahmi ، Ghadamali - Isfahan University of Medical Sciences , Rahmani Khajouei ، Marzieh - Isfahan University of Medical Sciences , Hassanzadeh ، Farshid - Isfahan University of Medical Sciences , Dana ، Nasim - Isfahan University of Medical Sciences
Abstract :
lt;p gt;Quinazolinone and benzimidazole are both fused heterocyclic compounds which have shown valuable biological properties including cytotoxic, antibacterial, and antifungal activities. In this study, a series of novel quinazolinone derivatives substituted with benzimidazole were synthesized in two parts. In the first part 2 phenyl 1 lt;em gt;H lt;/em gt; benzimidazol 6 amine ( lt;strong gt;4 lt;/strong gt;) was synthesized from the reaction of 4nitroophenylenediamine and benzoic acid. In the second part, new 3(2phenyl1 lt;em gt;H lt;/em gt; benzoimidazol5yl)3Hquinazolin4one derivatives ( lt;strong gt;8a8f lt;/strong gt;) were also prepared. Finally compound lt;strong gt;4 lt;/strong gt; was reacted with the different benzoxazinone derivatives ( lt;strong gt;8a8f lt;/strong gt;) to give the target compounds. The structures of the synthesized compounds were confirmed by IR and lt;sup gt;1 lt;/sup gt;HNMR. Cytotoxic activities of the final compounds were assessed at 100, 200, 300, 400, and 500 μM against MCF7 and HeLa cell lines using the MTT colorimetric assay. Almost all compounds exhibited good cytotoxic activity against both cell lines. Compound lt;strong gt;9d lt;/strong gt; demonstrated the highest cytotoxic activity against MCF7 and Hela cell lines with IC lt;sub gt;50 lt;/sub gt; 70 μM and 50 μM, respectively. lt;/p gt;
Keywords :
Cytotoxicity , Benzimidazole , MTT assay , Quinazolinone.
Journal title :
Research in Pharmaceutical Sciences
Journal title :
Research in Pharmaceutical Sciences