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Solvent-free synthesis and anticancer activity evaluation of benzimidazole and perimidine derivatives

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Abstract

Benzimidazoles and perimidines are subsidiary structures for research and development of new biologically active molecules and have established prominence because of their promising biological activities. Two series of diversified heterocyclic molecules, tetracyclic benzimidazole derivatives, tetracyclic and pentacyclic perimidine derivatives have been synthesized in good yields by condensation of acid anhydrides and diacids with various diamines using microwave irradiation. All synthesized derivatives were fully characterized and evaluated for in vitro antiproliferative activity against five human cancer cell lines. Compounds 3a (breast T47D, lung NCl H-522), 3b (colon HCT-15), 3d (lung NCl H-522, ovary PA-1), 3f (breast T47D, liver HepG2) and 5a (breast T47D) exhibited good anticancer activity with \(\hbox {IC}_{50}\) values ranging from \(7.5\pm 0.3\,\upmu \hbox {M}\) to \(14.6\pm 0.4\,\upmu \hbox {M}\).

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Acknowledgements

We are thankful to technical staff of the Chemistry Department, I. I. T. Roorkee, for spectroscopic studies and elemental analysis. Mr. Anuj Kumar is thankful to MHRD, New Delhi, for financial assistance.

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Authors and Affiliations

  1. Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee, Uttarakhand, 247667, India

    Anuj Kumar, S. M. Sondhi & Anuj Sharma

  2. Department of Biotechnology, Indian Institute of Technology Roorkee, Roorkee, Uttarakhand, 247667, India

    Somesh Banerjee & Partha Roy

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  1. Anuj Kumar
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Correspondence to Anuj Sharma.

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Kumar, A., Banerjee, S., Roy, P. et al. Solvent-free synthesis and anticancer activity evaluation of benzimidazole and perimidine derivatives. Mol Divers 22, 113–127 (2018). https://doi.org/10.1007/s11030-017-9790-3

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