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Synthesis, optical properties, and antioxidant and anticancer activity of benzoheterazole dendrimers with triazole bridging unit

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Abstract

Triazole-bridged benzoheterazole dendrimers with a bisphenol/benzophenone core unit have been synthesized by click chemistry via a convergent approach. The optical properties of the benzoheterazole dendrimers and their modulation under the influence of the dendritic environment are investigated. All the synthesized benzoheterazole dendrimers show antioxidant properties comparable to those of the standards, viz: gallic acid and ascorbic acid, when tested by DPPH and ABTS radical scavenging methods. Higher generation dendrimers exhibit superior antioxidant activity than the lower generation dendrimers due to the presence of a higher number of 1,2,3-triazole and benzophenone units. The therapeutic efficacy of the benzoheterazole dendrimers in inhibiting the growth of the A549 cancer cell increases as the dendritic generation increases. Our study shows that the inhibition of cell proliferation is dose and time dependent. MTT assay, cell viability, cell counting, and clonogenic assay indicate that the benzoheterazole dendrimers inhibit the growth of cancer cells, as revealed by reactive oxygen species and mitochondrial membrane potential studies. Morphological changes of the cancer cell line after treatment with the benzoheterazole dendrimers showed the typical features of cell death cell shrinkage and reduction in the number of cancer cells.

Graphical abstract: Synthesis, optical properties, and antioxidant and anticancer activity of benzoheterazole dendrimers with triazole bridging unit

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Publication details

The article was received on 20 Oct 2017, accepted on 18 Jan 2018 and first published on 19 Jan 2018


Article type: Paper
DOI: 10.1039/C7NJ04060A
Citation: New J. Chem., 2018, Advance Article
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    Synthesis, optical properties, and antioxidant and anticancer activity of benzoheterazole dendrimers with triazole bridging unit

    K. Rajavelu, M. Subaraja and P. Rajakumar, New J. Chem., 2018, Advance Article , DOI: 10.1039/C7NJ04060A

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