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Synthesis, characterization and biological evaluation of 7-substituted- 4-((1-aryl-1H-1,2,3-triazol-4-yl) methyl)-2H-benzo[b][1,4]oxazin- 3(4H)-ones as anticancer agents

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Abstract

A series of novel 1,2,3-triazole-2H-benzo[b][1,4]oxazin-3(4H)-ones (4a–4k and 5a–5g) were designed, synthesized and screened for their anticancer activity against MCF-7 (breast) and HeLa (cervical) cell lines using [3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide] assay. Among all the tested compounds, 5b and 5c exhibited good cytotoxic activity against two cancer cell lines with IC50 values nearer to the standard drug, cisplatin. The most active compounds 5b and 5c were further evaluated for their in vivo anticancer activity against Ehrlich Ascites Carcinoma-bearing mice and compound 5c found to possess potential cytotoxic activity as compared with the reference drug cisplatin. Molecular docking studies were also carried out to complement the experimental results.

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Acknowledgments

Financial assistance from the UGC-MRP (F.No. 42-372/2013), New Delhi, India, is greatly acknowledged. Narsimha and Satheesh are thankful to the Council of Scientific and Industrial Research-University Grant Commission (CSIR-UGC, New Delhi) for the award of senior research fellowship.

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Authors and Affiliations

  1. Department of Chemistry, Kakatiya University, Warangal, 506009, India

    Vasudeva Reddy Nagavelli, Satheesh Kumar Nukala, Sirassu Narsimha, Kumara Swamy Battula & Savitha Jyostna Tangeda

  2. Department of Pharmacology and Toxicology, Kakatiya University, Warangal, 506009, India

    Yellu Narasimha Reddy

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  1. Vasudeva Reddy Nagavelli
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  2. Satheesh Kumar Nukala
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Correspondence to Vasudeva Reddy Nagavelli.

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Nagavelli, V.R., Nukala, S.K., Narsimha, S. et al. Synthesis, characterization and biological evaluation of 7-substituted- 4-((1-aryl-1H-1,2,3-triazol-4-yl) methyl)-2H-benzo[b][1,4]oxazin- 3(4H)-ones as anticancer agents. Med Chem Res 25, 1781–1793 (2016). https://doi.org/10.1007/s00044-016-1616-9

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