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  • Synthesis of tetrazole-isoxazoline hybrids as a new class of tubulin polymerization inhibitors

    Author(s)
    Kamal, Ahmed
    Viswanath, Arutla
    Ramaiah, M. Janaki
    Murty, J. NSRC
    Sultana, Farheen
    Ramakrishna, Gajula
    Tamboli, Jaki R.
    Pushpavalli, Sreerangam N.C.V.L.
    Pal, Dhananjaya
    Kishor, Chandan
    Addlagatta, Anthony
    Bhadra, Manika P.
    Griffith University Author(s)
    Kishor, Chandan
    Year published
    2012
    Metadata
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    Abstract
    A new series of tetrazole based isoxazolines (4a–l) was synthesized and evaluated for their anticancer potential against two cancer cell lines. All these compounds exhibited profound cytotoxicity with IC50 values ranging from 1.22 to 3.62 μM and compounds 4h, 4i showed prominent anticancer efficacy with IC50 values of 1.51, 1.49 μM in A549 and 2.83, 2.40 μM in MDA-MB-231 cell lines. Further, these compounds (4h, 4i) induced apoptotic cell death by inhibition of tubulin polymerization leading to cell cycle arrest at G2/M phase of the cell cycle followed by caspase-3 activity. Moreover, the level of tubulin inhibition by these ...
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    A new series of tetrazole based isoxazolines (4a–l) was synthesized and evaluated for their anticancer potential against two cancer cell lines. All these compounds exhibited profound cytotoxicity with IC50 values ranging from 1.22 to 3.62 μM and compounds 4h, 4i showed prominent anticancer efficacy with IC50 values of 1.51, 1.49 μM in A549 and 2.83, 2.40 μM in MDA-MB-231 cell lines. Further, these compounds (4h, 4i) induced apoptotic cell death by inhibition of tubulin polymerization leading to cell cycle arrest at G2/M phase of the cell cycle followed by caspase-3 activity. Moreover, the level of tubulin inhibition by these compounds was examined by in vitro HTS tubulin polymerization assay. Docking of compound 4h and 4i to the active site of tubulin revealed that the trimethoxy ring of the compounds occupies the colchicine binding site of tubulin, whereas the isoxazoline moiety moves towards the interface of α–β tubulin and involves a series of hydrogen bonds with αTyr224 and αSer178.
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    Journal Title
    MedChemComm
    Volume
    3
    Issue
    11
    DOI
    https://doi.org/10.1039/c2md20085f
    Subject
    Medicinal and Biomolecular Chemistry not elsewhere classified
    Medicinal and Biomolecular Chemistry
    Organic Chemistry
    Pharmacology and Pharmaceutical Sciences
    Publication URI
    http://hdl.handle.net/10072/347865
    Collection
    • Journal articles

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