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Synthesis and Biological Evaluation of Theophylline Methyl 1,3,4-Oxadiazole as Anticancer Agents

Abstract

A series of theophylline methyl 1,3,4-oxadiazole small molecules were obtained via cyclization of theophylline-7-acetohydrazide with different benzoic acids. The compounds (IVaj) were synthesized and characterized by using conventional methods. The new compounds obtained were evaluated for their cytotoxic effect in three different cancer lines, the activity obtained varies depending upon the structure of a molecule. The compound (IVb) and (IVf) showed promising effect than other compounds of the series. Thus, these two derivatives have the potential for developing as anticancer agents.

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ACKNOWLEDGMENTS

We thank members of SCR and KSR laboratories for critical reading of the manuscript.

Funding

This work was supported by grants from IISc-DBT partnership program (DBT/BF/PR/INS/2011-12/IISc) for SCR. UR (09/079(2680)/2015-EMR-I) and VKG (no. 09/119(0200)/2015-EMR-I) are supported by Senior Research Fellowship from CSIR, Delhi, India.

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Correspondence to Kanchugarakoppal S. Rangappa.

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This article does not contain any studies involving human participants performed by any of the authors and does not contain any studies involving animals performed by any of the authors.

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The authors declare that they have no conflicts of interest.

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Corresponding author: e-mail: rangappaks@gmail.com.

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Vindya K. Gopinatha, Ray, U., Mantelingu, K. et al. Synthesis and Biological Evaluation of Theophylline Methyl 1,3,4-Oxadiazole as Anticancer Agents. Russ J Bioorg Chem 46, 837–844 (2020). https://doi.org/10.1134/S106816202005009X

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  • DOI: https://doi.org/10.1134/S106816202005009X

Keywords:

  • theophylline
  • cytotoxicity
  • oxadiazole
  • cancer