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    Synthesis and anticancer evaluation of spermatinamine analogues

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    Type
    Article
    Authors
    Moosa, Basem cc
    Sagar, Sunil
    Li, Song cc
    Esau, Luke
    Kaur, Mandeep
    Khashab, Niveen M. cc
    KAUST Department
    Advanced Membranes and Porous Materials Research Center
    Biological and Environmental Sciences and Engineering (BESE) Division
    Biomolecular Lab
    Chemical Science Program
    Computational Bioscience Research Center (CBRC)
    Computer, Electrical and Mathematical Sciences and Engineering (CEMSE) Division
    NGS, qPCR and Single Cell Genomics
    Office of the VP
    Physical Science and Engineering (PSE) Division
    Sanger and Third Generation Sequencing
    Smart Hybrid Materials (SHMs) lab
    Technology Transfer
    Date
    2016-02-04
    Online Publication Date
    2016-02-04
    Print Publication Date
    2016-03
    Permanent link to this record
    http://hdl.handle.net/10754/595859
    
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    Abstract
    Spermatinamine was isolated from an Australian marine sponge, Pseudoceratina sp. as an inhibitor of isoprenylcystiene carboxyl methyltransferase (Icmt), an attractive and novel anticancer target. Herein, we report the synthesis of spermatinamine analogues and their cytotoxic evaluation against three human cancer cell lines i.e. cervix adenocarcinoma (HeLa), breast adenocarcinoma (MCF-7), and prostate carcinoma (DU145). Analogues 12, 14 and 15 were found to be the most potent against one or more cell lines with the IC50 values in the range of 5 - 10 μM. The obtained results suggested that longer polyamine linker along with aromatic oxime substitution provided the most potent analogue compounds against cancer cell lines.
    Citation
    Synthesis and anticancer evaluation of spermatinamine analogues 2016 Bioorganic & Medicinal Chemistry Letters
    Publisher
    Elsevier BV
    Journal
    Bioorganic & Medicinal Chemistry Letters
    DOI
    10.1016/j.bmcl.2016.01.083
    PubMed ID
    26874403
    Additional Links
    http://linkinghub.elsevier.com/retrieve/pii/S0960894X16300919
    ae974a485f413a2113503eed53cd6c53
    10.1016/j.bmcl.2016.01.083
    Scopus Count
    Collections
    Articles; Biological and Environmental Science and Engineering (BESE) Division; Advanced Membranes and Porous Materials Research Center; Physical Science and Engineering (PSE) Division; Controlled Release and Delivery Laboratory; Chemical Science Program; Computational Bioscience Research Center (CBRC); Computer, Electrical and Mathematical Science and Engineering (CEMSE) Division

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