Design, synthesis, and anticancer properties of novel benzophenone- conjugated coumarin analogs

Lakshmi Ranganatha, V. and Zameer, F. and Meghashri, S. and Rekha, N. D. and Girish, V. and Gurupadaswamy, H. D. and Shaukath Ara Khanum (2013) Design, synthesis, and anticancer properties of novel benzophenone- conjugated coumarin analogs. Archiv der Pharmazie, 346 (12). pp. 901-911. ISSN 0365-6233

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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. 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.

Item Type:	Article
Uncontrolled Keywords:	2 oxo 2h chromene 3 carboxylic acid n' 2 (4 benzoyl 2, 2 oxo 2h chromene 3 carboxylic acid n' 2 (4 benzoyl 2 methylphenoxy)acetyl]hydrazide, 2 oxo 2h chromene 3 carboxylic acid n' 2 2 chloro 6 fluoro 4 (4 iodobenzoyl)phenoxy]acetyl]hydrazide, 2 oxo 2h chromene 3 carboxylic acid n' 2 2 chloro 6 fluoro 4 (4 methylbenzoyl)phenoxy]acetyl]hydrazide, 2 oxo 2h chromene 3 carboxylic acid n' 2 2 methyl 4 (2 methylbenzoyl) 2 methylphenoxy]acetyl]hydrazide, 2 oxo 2h chromene 3 carboxylic acid n' 2 2 methyl 4 (3 methylbenzoyl) 2 methylphenoxy]acetyl]hydrazide, 2 oxo 2h chromene 3 carboxylic acid n' 2 2 methyl 4 (4 fluorobenzoyl) 2 methylphenoxy]acetyl]hydrazide, 2 oxo 2h chromene 3 carboxylic acid n' 2 2 methyl 4 (4 methylbenzoyl) 2 methylphenoxy]acetyl]hydrazide, 2 oxo 2h chromene 3 carboxylic acid n' 2 4 (2, 2 oxo 2h chromene 3 carboxylic acid n' 2 4 (2 bromobenzoyl) 2 methylphenoxy]acetyl]hydrazide, 2 oxo 2h chromene 3 carboxylic acid n' 2 4 (2 chlorobenzoyl) 2 methylphenoxy]acetyl]hydrazide, 2 oxo 2h chromene 3 carboxylic acid n' 2 4 (3 chlorobenzoyl) 2 methylphenoxy]acetyl]hydrazide, 2 oxo 2h chromene 3 carboxylic acid n' 2 4 (4 bromobenzoyl) 2 methylphenoxy]acetyl]hydrazide, 2 oxo 2h chromene 3 carboxylic acid n' 2 4 (4 fluorobenzoyl) 2 methylphenoxy]acetyl]hydrazide, 2 oxo 2h chromene 3 carboxylic acid n' 2 4 (4 methoxybenzoyl) 2 methylphenoxy]acetyl]hydrazide, 6 dichlorobenzoyl) 2 methylphenoxy]acetyl]hydrazide, 6 dimethylphenoxy)acetyl]hydrazide, angiogenesis inhibitor, Angiogenesis Inhibitors, Animals, antiangiogenic activity, Anticancer agents, antineoplastic agent, Antineoplastic Agents, Apoptosis, article, Benzophenone, benzophenone derivative, Benzophenones, biological marker, CAM, Carcinoma, Caspase, caspase 3, caspase 8, Caspase Inhibitors, Caspases, Cell Proliferation, cell strain MCF 7, Chick Embryo, chorioallantois, computer model, Coumarin, coumarin derivative, Coumarins, cytotoxicity, DNA fragmentation, drug conjugation, drug design, Drug Design, drug protein binding, drug screening, drug synthesis, Ehrlich ascites tumor cell, Ehrlich Tumor, enzyme activation, enzyme inhibition, human, human cell, Humans, IC 50, in vivo study, Inhibitory Concentration 50, interleukin 1beta converting enzyme, MCF-7 Cells, Mice, Models, Molecular, molecular docking, Molecular Docking Simulation, Molecular Structure, Neovascularization, nonhuman, nucleotide sequence, phosphatidylinositol 3 kinase, Phosphatidylinositol 3-Kinase, Physiologic, PI3K, priority journal, prospective study, Protein Conformation, Signal Transduction, Structure-activity relation (SAR), Structure-Activity Relationship, tamoxifen, tumor model, unclassified drug
Subjects:	B Life Science > Biotechnology C Chemical Science > Chemistry
Divisions:	Department of > Biotechnology Yuvaraj college > Chemistry
Depositing User:	Arshiya Kousar Library Assistant
Date Deposited:	16 Oct 2019 09:42
Last Modified:	16 Oct 2019 09:42
URI:	http://eprints.uni-mysore.ac.in/id/eprint/8963

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