20.500.12556/RUL-141908 Synthesis, antiproliferative effect and topoisomerase II inhibitory activity of 3-methyl-2-phenyl-1H-indoles 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. 3-Methyl-2-phenyl-1H-indole antiproliferative activity topoisomerase II apoptosis apoptoza rak (medicina) true false true Angleški jezik Slovenski jezik Članek v reviji 2022-10-11 11:43:36 2022-10-11 11:43:37 2022-10-12 03:52:41 0000-00-00 00:00:00 2020 0 0 Str. 691-697 iss. 5 Vol. 11 2020 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 576.36: 615.4:54 1948-5875 10.1021/acsmedchemlett.9b00557 4874609 acsmedchemlett.9b00557.pdf acsmedchemlett.9b00557.pdf 1 30CED5F93CB8E60D331E2311726734C0 b20e19141434dd2ed0bbee251f5be15b8be5a1943d92e31dc7db3e2e2c8c83a1 72aa4496-4949-11ed-9c94-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=163085 https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.9b00557 1 25abec2b-4949-11ed-9c94-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=163083 https://pubs.acs.org/doi/10.1021/acsmedchemlett.9b00557 1 2591ba80-4949-11ed-9c94-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=163082 Fakulteta za farmacijo 0 0 0