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Design and Synthesis of Novel 2-Substituted-Benzyl-5-(2-Methylbenzofuran-3-yl)-2H-Tetrazoles: Anti-Proliferative Activity

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Abstract

A new series of 2,5-regioselective benzofuran-tetrazole hybrids (XIIIa–XIIIp) were synthesised from 2H-chromene-3-carbonitriles (IXa), (IXb) in multi steps approach under mild reaction conditions in good yields and evaluated their anti-proliferative activity against HCT116 and Miapaca2 cell lines. Wherein compounds (XIIIe) (IC50: 3.19 μM) and (XIIIm) (IC50: 2.25 μM) were displayed highest anti-proliferative activity in both cell lines. Molecular docking and SAR studies revealed the in vitro results with target Proto-oncogene tyrosine kinase Src protein.

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ACKNOWLEDGMENTS

MS thanks to the UGC-New Delhi, India, for providing UGC-SRF fellowship, Head Department of Chemistry and CFRD Osmania University, Hyderabad, India for providing facilities.

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Authors and Affiliations

  1. Natural Products Laboratory, Department of Chemistry, Osmania University, 500007, Hyderabad, Telangana, India

    Sudhakar Mokenapelli, Madhu Gutam, Jayaprakash Rao Yerrabelli & Prasad Rao Chitneni

  2. Department of Genetics and Biotechnology, Osmania University, 500007, Hyderabad, Telangana, India

    Vamshi Krishna Irlapati, Neelima Gorityala & Someswar Rao Sagurthi

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  1. Sudhakar Mokenapelli
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Correspondence to Prasad Rao Chitneni.

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Sudhakar Mokenapelli, Gutam, M., Yerrabelli, J.R. et al. Design and Synthesis of Novel 2-Substituted-Benzyl-5-(2-Methylbenzofuran-3-yl)-2H-Tetrazoles: Anti-Proliferative Activity. Russ J Bioorg Chem 46, 845–855 (2020). https://doi.org/10.1134/S1068162020050179

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