Synthesis and pharmacological evaluation of novel bisindolylalkanes analogues |
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| Authors: | Ya-Li Song Yun-Fang Dong Tao Yang Chao-Chao Zhang Li-Min Su Xin Huang Dong-Nuan Zhang Geng-Liang Yang Yu-Xin Liu |
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| Affiliation: | 1. Key Laboratory for Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Wusi East Road No. 180, Baoding, Hebei 071002, China;2. Key Laboratory of Medical Chemistry and Molecular Diagnosis, Ministry of Education, Wusi East Road No. 180, Baoding, Hebei 071002, China;3. College of Science, Agricultural University of Hebei, Baoding, Hebei 071001, China |
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| 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 1H NMR, 13C 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. |
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| Keywords: | Bisindolylalkane Anticancer Topoisomerase II Indole Thiochroman-4-one |
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