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Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel 1,2,3-Triazole Tagged 5-[(1H-Indol-3-yl)methylene]pyrimidine-2,4,6(1H,3H,5H)trione Derivatives

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Abstract

Novel 5-{(1-[(1-phenyl-1H-1,2,3-triazol-4-yl)methyl]-1H-indol-3-yl)methylene}pyrimidine-2,4,6-(1H,3H,5H)trione derivatives (5a–5k) were synthesized by the click reaction. All compounds 5a–5k were characterized by 1H and 13C NMR, IR and Mass spectra and evaluated for their in vitro anticancer activity against cervical cancer cell lines. Among all, compound 5e (IC50 = 6.76 μM), shown high inhibitory activity. Docking analysis of all the compounds with the Lipid kinase PI3K-α revealed that the compound 5e fitted well in the active site pocket, showing the best docking score (LibDock) of 123.274.

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Authors and Affiliations

  1. Department of Chemistry, Sreenidhi Institute of Science and Technology, Yamnampet, Ghatkesar, Hyderabad, Telangana, 501301, India

    Ashok Kumar

  2. Department of Chemistry, Osmania University, Hyderabad, Telangana, 500007, India

    B. Sathish Kumar

  3. Bioinformatics Division, Averin Biotech Pvt. Ltd. Windsorplaza, Nallakunta, Hyderabad, Telangana, 500044, India

    E. Sreenivas

  4. Department of Chemistry, Koneru Lakshmaiah Deemed to be University, Green Fields, Vaddeswaram, Guntur (Dist), Andhra Pradesh, 522502, India

    Ashok Kumar & T. Subbaiah

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  1. Ashok Kumar
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  2. B. Sathish Kumar
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  3. E. Sreenivas
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  4. T. Subbaiah
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Correspondence to Ashok Kumar.

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Kumar, A., Sathish Kumar, B., Sreenivas, E. et al. Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel 1,2,3-Triazole Tagged 5-[(1H-Indol-3-yl)methylene]pyrimidine-2,4,6(1H,3H,5H)trione Derivatives. Russ J Gen Chem 88, 587–595 (2018). https://doi.org/10.1134/S1070363218030313

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  • DOI: https://doi.org/10.1134/S1070363218030313

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