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    Synthesis and Evaluation of Novel Carboxamides Capable of Causing Centrosome Declustering and Apoptosis in Breast Cancer Cells

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    Type
    Article
    Authors
    Farrukh, Usama B.
    Bilal, Aishah
    Zahid, Huda cc
    Iqbal, Maheen
    Manzoor, Safia
    Firdous, Farhat
    Furqan, Muhammad
    Azeem, Muhammad
    Emwas, Abdul-Hamid M. cc
    Alazmi, Meshari cc
    Gao, Xin cc
    Zaib Saleem, Rahman Shah cc
    Faisal, Amir
    KAUST Department
    Computer, Electrical and Mathematical Sciences and Engineering Division King Abdullah University of Science and Technology Thuwal 23955-6900, Kingdom of Saudi Arabia
    Structural and Functional Bioinformatics Group
    Computer Science Program
    Computer, Electrical and Mathematical Science and Engineering (CEMSE) Division
    Computational Bioscience Research Center (CBRC)
    Imaging and Characterization Core Lab
    Date
    2022-04-19
    Embargo End Date
    2023-04-19
    Permanent link to this record
    http://hdl.handle.net/10754/676393
    
    Metadata
    Show full item record
    Abstract
    The fragility of cancer cells at the time of mitosis has served as an important target for the development of many successful chemotherapeutic agents. Many cancers cells have supernumerary centrosomes that they cluster during mitosis to form bipolar spindles. Inhibition of centrosome clustering in these cells results in multipolar spindle formation and apoptotic cell death, providing an opportunity to selectively target a subset of cancers with centrosome amplification. In the current work, we report synthesis of 29 novel tethered biaryls and biological evaluation of their ability to inhibit centrosome clustering in breast cancer cells (BT-549). We have identified N-benzhydryl-5-nitrofuran-2-carboxamide (5 h) as a centrosome declustering compound. 5 h has potent antiproliferative activity in centrosome amplified BT-549 cells with GI50 value of 1.81±0.19 μM (n=2). Treatment of BT-549 cells with 5 h causes centrosome declustering resulting in mitotic arrest due to multipolar spindle formation and misaligned chromosomes which ultimately leads to apoptotic cell death
    Citation
    Farrukh, U. B., Bilal, A., Zahid, H., Iqbal, M., Manzoor, S., Firdous, F., Furqan, M., Azeem, M., Emwas, A., Alazmi, M., Gao, X., Saleem, R. S. Z., & Faisal, A. (2022). Synthesis and Evaluation of Novel Carboxamides Capable of Causing Centrosome Declustering and Apoptosis in Breast Cancer Cells. ChemistrySelect, 7(15). Portico. https://doi.org/10.1002/slct.202104218
    Sponsors
    Supported by Higher Education Commission, Pakistan (NRPU-5914) and LUMS Faculty Initiative Funds (FIF-222 and FIF-533)
    Publisher
    Wiley
    Journal
    ChemistrySelect
    DOI
    10.1002/slct.202104218
    Additional Links
    https://onlinelibrary.wiley.com/doi/10.1002/slct.202104218
    ae974a485f413a2113503eed53cd6c53
    10.1002/slct.202104218
    Scopus Count
    Collections
    Articles; Imaging and Characterization Core Lab; Structural and Functional Bioinformatics Group; Computer Science Program; Computational Bioscience Research Center (CBRC); Computer, Electrical and Mathematical Science and Engineering (CEMSE) Division

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