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  • Synthesis, antiproliferative effect and topoisomerase II inhibitory activity of 3-methyl-2-phenyl-1H-indoles
    Zidar, Nace ...
    A series of 3-methyl-2-phenyl-1H-indoles was prepared and investigated for antiproliferative activity on three human tumor cell lines, HeLa, A2780, and MSTO-211H, and some structure-activity ... relationships were drawn up. The GI50 values of the most potent compounds (32 and 33) were lower than 5 [micro]M in all tested cell lines. For the most biologically relevant derivatives, the effect on human DNA topoisomerase II relaxation activity was investigated, which highlighted the good correlation between the antiproliferative effect and topoisomerase II inhibition. The most potent derivative, 32, was shown to induce the apoptosis pathway. The obtained results highlight 3-methyl-2-phenyl-1H-indole as a promising scaffold for further optimization of compounds with potent antiproliferative and antitopoisomerase II activities.
    Source: ACS Medicinal Chemistry Letters. - ISSN 1948-5875 (Vol. 11, iss. 5, 2020, str. 691-697)
    Type of material - article, component part
    Publish date - 2020
    Language - english
    COBISS.SI-ID - 4874609

    Link(s):

    https://pubs.acs.org/doi/10.1021/acsmedchemlett.9b00557
    https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.9b00557
    Repository of the University of Ljubljana – RUL
    DOI

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