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Synthesis and Biological Evaluation of Novel 1,2,3-Triazole Based Pyrido[4,3-d]pyrimidines as Potent Anticancer and EGFR Inhibitors

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Abstract

This study is devoted to the efficient and practical synthesis of a novel series of pyrido[4,3-d]pyrimidine derivatives attached to 1,2,3-triazole ring and lipophilic terminal fractions. Structure of the newly synthesized compounds is well characterized by various spectroscopic methods. An in vitro MTT cytotoxicity assay has been used to compare cytotoxic effects of the synthesized compounds on MCF-7, HeLa, and A-549. The kinase inhibitory assay against tyrosine kinase EGFR has been performed for the potent compounds and the results are supporting their in vitro anticancer activity. Further study of their binding affinity has been performed by molecular docking with the EGFR site. The molecular docking and cytotoxic tests results correlate well.

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ACKNOWLEDGMENTS

The authors are thankful to the head, Department of Biotechnology, Chaitanaya Deemed to be University, Warangal, for providing data of biological activity.

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Authors and Affiliations

  1. Department of Chemistry, Chaitanya Deemed to be University, Warangal, 506001, Telangana, India

    Rakesh Sreerama, N. Manoj Kumar, Satheesh Kumar Nukala, E. Ramya Sucharitha & Sirassu Narsimha

  2. epartment of Physical Sciences/Chemistry, Kakatiya Institute of Technology and Science (A), Warangal, 506015, Telangana, India

    H. Ramesh Babu

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  1. Rakesh Sreerama
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  2. N. Manoj Kumar
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  3. Satheesh Kumar Nukala
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  4. E. Ramya Sucharitha
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  6. Sirassu Narsimha
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Correspondence to Sirassu Narsimha.

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Sreerama, R., Kumar, N.M., Nukala, S.K. et al. Synthesis and Biological Evaluation of Novel 1,2,3-Triazole Based Pyrido[4,3-d]pyrimidines as Potent Anticancer and EGFR Inhibitors. Russ J Gen Chem 91, 2515–2521 (2021). https://doi.org/10.1134/S1070363221120227

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  • DOI: https://doi.org/10.1134/S1070363221120227

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