Design and Synthesis of Novel Pyrazolo[3,4-d]Pyrimidines: In Vitro Cytotoxic Evaluation and Free Radical Scavenging Activity Studies

With evident biological importance, a new series of pyrazolo[3,4-d]pyrimidines 3a,3b and 4a,4b were synthesized via the formation of pyrazol-3-one 2a and 2b substrates. All compounds were evaluated for in vitro cytotoxic activity against MCF-7 (breast adenocarcinoma) and A549 (lung cancer) cell lines. The obtained results showed that pyrazolo[3,4-d] pyrimidin-4-ol 3a bearing phenyl group at N-1 and p-C6H4 at C-6, and 4b with dinitrophenyl at N-1 and furanyl moiety at C-6 had better inhibitory activity against MCF-7 with IC50 values in a micromolar range as compared to other substrates. The synthesized compounds can be considered as new candidates for further optimization as anticancer agents.

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Acknowledgements

The authors are thankful to the Deanship of Scientific Research, King Abdulaziz University, Jeddah, Saudi Arabia (grant number, G-1436-363-328) for great support of this work.

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Author declares no conflicts of interest.

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Correspondence to Rima D. Alharthy.

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Alharthy, R.D. Design and Synthesis of Novel Pyrazolo[3,4-d]Pyrimidines: In Vitro Cytotoxic Evaluation and Free Radical Scavenging Activity Studies. Pharm Chem J 54, 273–278 (2020). https://doi.org/10.1007/s11094-020-02190-2

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Keywords

  • pyrazolo[3,4-d]pyrimidines
  • pharmacophore
  • cytotoxicity
  • anticancer
  • radical scavenging activity