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    Synthesis of novel 1H-1,2,3-triazole tethered C-5 substituted uracil-isatin conjugates and their cytotoxic evaluation

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    Type
    Article
    Authors
    Kumar, Kewal
    Sagar, Sunil
    Esau, Luke
    Kaur, Mandeep
    Kumar, Vipan
    KAUST Department
    Computational Bioscience Research Center (CBRC)
    Computer, Electrical and Mathematical Sciences and Engineering (CEMSE) Division
    Technology Transfer
    Date
    2012-12
    Permanent link to this record
    http://hdl.handle.net/10754/562442
    
    Metadata
    Show full item record
    Abstract
    The present manuscript describes the synthesis of uracil-isatin hybrids via azide-alkyne cycloadditions and their cytotoxic evaluation against three human cancer cell lines viz. HeLa (cervix), MCF-7 (breast) and DU145 (prostate) using MTT assay. The evaluation studies revealed the dependence of cytotoxicity on C-5 substituents of both uracil and isatin as well as the alkyl chain length with compounds 6g and 6k showing IC50 values 18.21 and 13.90 μM respectively against DU145 cell lines. Most of the synthesized conjugates exhibited considerable selectivity against MCF-7 and DU145 cell lines. © 2012 Elsevier Masson SAS. All rights reserved.
    Citation
    Kumar, K., Sagar, S., Esau, L., Kaur, M., & Kumar, V. (2012). Synthesis of novel 1H-1,2,3-triazole tethered C-5 substituted uracil–isatin conjugates and their cytotoxic evaluation. European Journal of Medicinal Chemistry, 58, 153–159. doi:10.1016/j.ejmech.2012.10.008
    Sponsors
    Financial assistance from Department of Science and Technology, New Delhi under Innovation in Science Pursuit for Inspired Research (INSPIRE) Fellowship (KK) is gratefully acknowledged.
    Publisher
    Elsevier BV
    Journal
    European Journal of Medicinal Chemistry
    DOI
    10.1016/j.ejmech.2012.10.008
    PubMed ID
    23124212
    ae974a485f413a2113503eed53cd6c53
    10.1016/j.ejmech.2012.10.008
    Scopus Count
    Collections
    Articles; Computational Bioscience Research Center (CBRC); Computer, Electrical and Mathematical Science and Engineering (CEMSE) Division

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