title: Design, synthesis, and anticancer properties of novel benzophenone-conjugated coumarin analogs.
abstract: 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.
authors.affiliation: Department of Chemistry, Yuvaraja's College, University of Mysore, Mysore, Karnataka, India.
authors.forename: V
authors.initials: V
authors.lastname: Lakshmi Ranganatha
authors.forename: Farhan
authors.initials: F
authors.lastname: Zameer
authors.forename: S
authors.initials: S
authors.lastname: Meghashri
authors.forename: N D
authors.initials: ND
authors.lastname: Rekha
authors.forename: V
authors.initials: V
authors.lastname: Girish
authors.forename: H D
authors.initials: HD
authors.lastname: Gurupadaswamy
authors.forename: Shaukath Ara
authors.initials: SA
authors.lastname: Khanum
mesh_terms: D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001577:Benzophenones / Q000138:chemical synthesis* / Q000494:pharmacology*; D002286:Carcinoma, Ehrlich Tumor / Q000378:metabolism / Q000473:pathology; D061945:Caspase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D020169:Caspases / Q000737:chemistry / Q000378:metabolism; D049109:Cell Proliferation / Q000187:drug effects; D002642:Chick Embryo; D003374:Coumarins / Q000138:chemical synthesis* / Q000494:pharmacology*; 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 / Q000187:drug effects; D058539:Phosphatidylinositol 3-Kinase / Q000737:chemistry / Q000378:metabolism; D011487:Protein Conformation; D015398:Signal Transduction / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D001577:Benzophenones; D061945:Caspase Inhibitors; D003374:Coumarins; C047723:benzophenone; C030123:coumarin; D058539:Phosphatidylinositol 3-Kinase; D020169:Caspases
keywords: Anticancer agents; Benzophenone; CAM; Caspase; Coumarin; PI3K; Structure-activity relation (SAR)