Design, synthesis and biological screening of pyrazole and pyrazolopyrimidine derivatives as anticancer agents /
تصميم و تشييد و مسح بيولوجى لمشتقات البيرازول و البيرازولوبيريميدين كمضادات للسرطان
Esraa Abdelmoneim Abdelmajeed Mostafa ; Supervised Ghaneya S. Hassan , Doaa E. Abdelrahman , Yassin M. Nissan
- Cairo : Esraa Abdelmoneim Abdelmajeed Mostafa , 2017
- 144 P. : photographs ; 25cm
Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry
Cancer is the second leading cause of death after cardiovascular complication with expectation of being first in coming few years. Accordingly, continued research is needed to develop new antitumor agents. Pyrazole or pyrazolopyrimidine scaffold is a very interesting bioactive core exhibiting several biological activities including anticancer, antimicrobial, antioxidant, antifungal and anti-inflammatory activities. In addition, sulfonamide functional moiety possessed good anticancer activity. Accordingly, new pyrazole or pyrazolopyrimidine derivatives bearing benzenesulfonamide moiety were designed and synthesized. The cytotoxic activities of the synthesized compounds against liver cancer cell line (HepG2) and breast cancer cell line (MCF7) were investigated. In addition, in vitro cell cycle analysis, apoptosis with its marker (caspase-3) and cyclin dependent kinase with its regulators (p21 and p27) were performed against the highly active compound to elucidate the possible mechanism of action. Furthermore molecular docking was established to predict the possible binding mode between the most active compound and the binding site in active site