title: Synthesis and pharmacological evaluation of novel bisindolylalkanes analogues.
abstract: 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.
authors.affiliation: Key Laboratory for Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Wusi East Road No. 180, Baoding, Hebei 071002, China; Key Laboratory of Medical Chemistry and Molecular Diagnosis, Ministry of Education, Wusi East Road No. 180, Baoding, Hebei 071002, China.
authors.forename: Ya-Li
authors.initials: YL
authors.lastname: Song
authors.forename: Yun-Fang
authors.initials: YF
authors.lastname: Dong
authors.forename: Tao
authors.initials: T
authors.lastname: Yang
authors.forename: Chao-Chao
authors.initials: CC
authors.lastname: Zhang
authors.forename: Li-Min
authors.initials: LM
authors.lastname: Su
authors.forename: Xin
authors.initials: X
authors.lastname: Huang
authors.forename: Dong-Nuan
authors.initials: DN
authors.lastname: Zhang
authors.forename: Geng-Liang
authors.initials: GL
authors.lastname: Yang
authors.forename: Yu-Xin
authors.initials: YX
authors.lastname: Liu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004250:DNA Topoisomerases, Type II / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D061986:MCF-7 Cells; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; D059005:Topoisomerase II Inhibitors; D004250:DNA Topoisomerases, Type II
keywords: Anticancer; Bisindolylalkane; Indole; Thiochroman-4-one; Topoisomerase II