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One Pot Synthesis and Antitumor Activity of Isoxazole-Pyrimido[4,5-c]isoquinolines

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Abstract

A number of new isoxazole coupled pyrimido[4,5-c]isoquinolines has been synthesized in good to excellent yields by the one pot method. The Cu(I)-catalyzed cycloaddition reaction between the terminal alkyne 4 and various aldehydes has led to nitrile oxides. The in vitro study of antitumor activity of the products has indicated three of those to be potent anticancer (MCF-7) agents with IC50 values close to that of the standard drug. Molecular docking studies have also been conducted to complement the experimental results.

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ACKNOWLEDGMENTS

The authors are thankful to the Director of Indian Institute of Chemical Technology in Hyderabad for recording 1H, 13C NMR, and mass spectra. The authors are thankful to the head, Department of Biotechnology, Kakatiya University, Warangal, for providing data of biological activity.

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Correspondence to N. V. Reddy.

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Venkatesh, E., Narsimha, S., Kumar, N.S. et al. One Pot Synthesis and Antitumor Activity of Isoxazole-Pyrimido[4,5-c]isoquinolines. Russ J Gen Chem 90, 2444–2450 (2020). https://doi.org/10.1134/S1070363220120361

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