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Synthesis , antitumor activity evaluation and DNA binding study of some novel coumarins and derived polycyclic ring systems /

Nada Mostafa Mohamed Mostafa Elsayed

Synthesis , antitumor activity evaluation and DNA binding study of some novel coumarins and derived polycyclic ring systems / تشييد و تقييم الفاعلية المضادة للأورام و دراسة الإرتباط بالحمض النووي لبعض الكومارينات الجديدة و مشتقاتها المتعددة الحلقات Nada Mostafa Mohamed Mostafa Elsayed ; Supervised Kamilia M. Amin , Aly M. Taha , Riham F. George - Cairo : Nada Mostafa Mohamed Mostafa Elsayed , 2018 - 156 P. : charts , facsimiles ; 25cm

Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry

Coumarin nucleus has been extensively studied in medicinal chemistry for its diverse pharmacological activities including anti-inflammatory, antibiotic, anticonvulsant, anticoagulant and antitumor activity. Therefore, its antitumor activity was considered during the synthesis of five novel series of substituted 6-aminocoumarin hybridized with five reported active moieties as antitumor. Those moieties were; schiffs, functionalized aryl, thiadiazole, cyclic secondary amines and fused tricyclic pyridocoumarin. Their antitumor activity was biologically evaluated through DNA interaction and against human cancerous cell lines. Most of the compounds had better DNA/ethidium bromide fluorescence quenching rather than methyl green displacement which suggested a superior DNA intercalation mode of action to DNA major groove binding



Antitumor and DNA-binding/cleavage Coumarin Thiadiazole