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Synthesis, Antiproliferative Effect, and Topoisomerase II Inhibitory Activity of 3-Methyl-2-phenyl-1H-indoles.

ABSTRACT: 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 μM 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.

SUBMITTER: Zidar N 

PROVIDER: S-EPMC7236043 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature

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Synthesis, Antiproliferative Effect, and Topoisomerase II Inhibitory Activity of 3-Methyl-2-phenyl-1<i>H</i>-indoles.

Zidar Nace N   Secci Daniela D   Tomašič Tihomir T   Mašič Lucija Peterlin LP   Kikelj Danijel D   Passarella Daniele D   Argaez Aida Nelly Garcia ANG   Hyeraci Mariafrancesca M   Dalla Via Lisa L  

ACS medicinal chemistry letters 20200124 5

A series of 3-methyl-2-phenyl-1<i>H</i>-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 GI<sub>50</sub> values of the most potent compounds (<b>32</b> and <b>33</b>) were lower than 5 μM in all tested cell lines. For the most biologically relevant derivatives, the effect on human DNA topoisomerase II relaxation activity was investigated, which highlighted  ...[more]

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