Design, synthesis, and anticancer properties of novel benzophenone-conjugated coumarin analogs.
In the current scenario, development of anticancer drugs with specific targets is of prime importance in modern chemical biology. Observing the importance of benzophenone and coumarin nucleus, it would be worthwhile to design and synthesize novel benzophenone derivatives (8a-o) bearing the coumarin nucleus. Further, they were screened for prospective anticancer activities in vitro against the Michigan Cancer Foundation-7 (MCF-7) and Ehrlich's ascites tumor (EAT) cell lines and their biomarkers, followed by in silico studies regarding phosphoinositide 3-kinase (PI3K) and caspase by molecular docking. Benzophenones have been reported as potential drugs targeting tumor angiogenesis; thus, the formation of neovessels in an in vivo model system like CAM, which is angiogenesis dependent, was observed in the presence of compounds 8a-o. The above findings would help in understanding their putative potential as therapeutic agents for cancer patients.
['Lakshmi Ranganatha|V|V|', 'Zameer|Farhan|F|', 'Meghashri|S|S|', 'Rekha|N D|ND|', 'Girish|V|V|', 'Gurupadaswamy|H D|HD|', 'Khanum|Shaukath Ara|SA|']
D020533:Angiogenesis Inhibitors D000818:Animals D000970:Antineoplastic Agents D017209:Apoptosis D001577:Benzophenones D002286:Carcinoma, Ehrlich Tumor D061945:Caspase Inhibitors D020169:Caspases D049109:Cell Proliferation D002642:Chick Embryo D003374:Coumarins D015195:Drug Design D006801:Humans D020128:Inhibitory Concentration 50 D061986:MCF-7 Cells D051379:Mice D008958:Models, Molecular D062105:Molecular Docking Simulation D015394:Molecular Structure D018919:Neovascularization, Physiologic D058539:Phosphatidylinositol 3-Kinase D011487:Protein Conformation D015398:Signal Transduction D013329:Structure-Activity Relationship
Coumarin Benzophenone PI3K Caspase CAM Anticancer agents Structure-activity relation (SAR)