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...

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Veröffentlicht in:Archiv der Pharmazie (Weinheim) 2013-12, Vol.346 (12), p.901-911
Hauptverfasser: Lakshmi Ranganatha, V., Zameer, Farhan, Meghashri, S., Rekha, N. D., Girish, V., Gurupadaswamy, H. D., Khanum, Shaukath Ara
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Sprache:eng
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Zusammenfassung: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. Coumarin‐integrated benzophenone conjugates (8a–o) were designed, synthesized, and screened for prospective anticancer activities in vitro against the MCF‐7 and EAT cell lines. Molecular docking studies with regard to phosphoinositide 3‐kinase and caspase were performed. In addition, neovessel formation was observed in an in vivo model system.
ISSN:0365-6233
1521-4184
DOI:10.1002/ardp.201300298