86111-12-8Relevant academic research and scientific papers
Synthesis, Antiproliferative Effect, and Topoisomerase II Inhibitory Activity of 3-Methyl-2-phenyl-1 H-indoles
Argaez, Aida Nelly Garcia,Dalla Via, Lisa,Hyeraci, Mariafrancesca,Kikelj, Danijel,Ma?i?, Lucija Peterlin,Passarella, Daniele,Secci, Daniela,Toma?i?, Tihomir,Zidar, Nace
, p. 691 - 697 (2020/07/14)
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.
2-Phenylindoles. Relationship between Structure, Estrogen Receptor Affinity, and Mammary Tumor Inhibiting Activity in the Rat
Angerer, Erwin von,Prekajac, Jelica,Strohmeier, Josef
, p. 1439 - 1447 (2007/10/02)
A number of 2-phenylindole derivatives with one hydroxy group in the meta or para position of the phenyl ring and a second one in position 5, 6, or 7 of the indole nucleus were synthesized.In addition, different alkyl groups were introduced into positions
