Synthesis and pharmacological evaluation of novel bisindolylalkanes analogues.
In an effort to develop potent anti-cancer chemopreventive agents that act on topoisomerase II, a novel series of bisindolylalkanes analogues such as 3,3'-(thiochroman-4,4-diyl)bis(1H-indole) are synthesized. Structures of all compounds are elucidated by (1)H NMR, (13)C NMR and HRMS. Anti-proliferative activities for all of these compounds are investigated by the method of MTT assay on 7 human cancer lines. Most of them showed antitumor activities in vitro, the half maximal inhibitory concentration (IC50) value is 7.798 μg/mL of 3a against MCF7. Compound 3a showed comparable topoisomerase II inhibitory activity to etoposide (VP-16) at 100 μM concentration. The rest of the compounds also showed varying degree topoisomerase II inhibitory activity.
['Song|Ya-Li|YL|', 'Dong|Yun-Fang|YF|', 'Yang|Tao|T|', 'Zhang|Chao-Chao|CC|', 'Su|Li-Min|LM|', 'Huang|Xin|X|', 'Zhang|Dong-Nuan|DN|', 'Yang|Geng-Liang|GL|', 'Liu|Yu-Xin|YX|']
D000970:Antineoplastic Agents D045744:Cell Line, Tumor D049109:Cell Proliferation D004250:DNA Topoisomerases, Type II D004305:Dose-Response Relationship, Drug D004354:Drug Screening Assays, Antitumor D056945:Hep G2 Cells D006801:Humans D007211:Indoles D020128:Inhibitory Concentration 50 D061986:MCF-7 Cells D015394:Molecular Structure D013329:Structure-Activity Relationship D059005:Topoisomerase II Inhibitors
Bisindolylalkane Topoisomerase II Anticancer Indole Thiochroman-4-one