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In vitro, in vivo and in silico-driven identification of novel benzimidazole derivatives as anticancer and anti-inflammatory agents

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Abstract

The synthesis of novel benzimidazole derivatives with varied carbon chain length was achieved via “one-pot” nitro reductive cyclization (6a–o). In each case, compounds were determined by the elemental analyses, FT-IR, mass, 1H and 13C NMR spectroscopy. Further, these derivatives were screened for their in vitro anticancer, in vitro and in vivo anti-inflammatory activities. The results revealed that the length of the carbon chain greatly affects the activity. Among the 15 derivatives, compound 6d induced maximum cell death in HeLa and A549 cell lines and compound 6a emerged as a potent anti-inflammatory agent. Also, the physicochemical properties of potent compounds were studied.

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Acknowledgements

The author thank DST/KSTePS, Karnataka, for providing Ph.D. Fellowship and thankful to DST-PURSE Laboratory, Mangalore University.

Funding

This research was funded by DST/KSTePS through fellowship (DST/KSTePS/Ph.D.Fellowship/CHE-07:2019-20/462/2).

Author information

Authors and Affiliations

  1. Department of Chemistry, Mangalore University, Mangalagangothri, Karnataka, 574199, India

    Reshma Sathyanarayana & Boja Poojary

  2. Adichunchanagiri Institute for Molecular Medicine, AIMS, Adichuncanagiri University, BG Nagara, Karnataka, 571448, India

    Sudhanva M. Srinivasa & Shobith Rangappa

  3. Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences Nitte University, Mangaluru, Karnataka, India

    Vijay K. Merugumolu & Revanasiddappa B. Chandrashekarappa

  4. Faculty of Natural Sciences, Adichuncanagiri University, BG Nagara, Karnataka, 571448, India

    Sudhanva M. Srinivasa & Shobith Rangappa

Authors
  1. Reshma Sathyanarayana
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  2. Boja Poojary
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  3. Sudhanva M. Srinivasa
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  4. Vijay K. Merugumolu
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  5. Revanasiddappa B. Chandrashekarappa
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Corresponding author

Correspondence to Boja Poojary.

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The authors declare that they have no conflict of interest.

Ethical approval

The experimental protocols according to the CPCSEA guidelines and IAEC clearance were taken prior to the commencement of the study. The animal treatment protocol was approved by Reg. No. NGSM/IAEC/March-2019/129.

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Supplementary file: This portion contains characterization. (DOCX 7316 kb)

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Sathyanarayana, R., Poojary, B., Srinivasa, S.M. et al. In vitro, in vivo and in silico-driven identification of novel benzimidazole derivatives as anticancer and anti-inflammatory agents. J IRAN CHEM SOC 19, 1301–1317 (2022). https://doi.org/10.1007/s13738-021-02381-y

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  • DOI: https://doi.org/10.1007/s13738-021-02381-y

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