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Design,synthesis and biological activities of tetrandrine and fangchinoline derivatives as antitumer agents
Authors:Dechao Li  Haizheng Liu  Yufa Liu  Qikun Zhang  Chao Liu  Shuhua Zhao  Bo Jiao
Institution:1. College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Center of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Provincial Key Laboratory of Clean Production of Fine Chemicals, Shandong Normal University, 88 East Wenhua Road, Jinan 250014, PR China;2. Institute of Agro-Food Science and Technology, Shandong Academy of Agricultural Sciences, 202 Gongye North Road, Jinan 250100, PR China;3. School of Medicine, Shandong University, 44 West Wenhua Road, Jinan 250012, PR China
Abstract:The isolation and modification of natural products is always a very important resources to anti-tumor drugs. Therefore, a novel series of tetrandrine and fangchinoline derivatives were designed and synthesized, and their antiproliferative activities against HepG2, MCF-7 cells were evaluated and described. From the activity result obtained, high to very high activity in vitro has been found, one of the tested compounds (compound 5d) exhibited the most significant cytotoxic effects. Compound 5d increased 29.2, 7.37 times anti-proliferative activity for HepG2 cells and MCF-7 cells compared to sunitinib (IC50 = 16.06 μM and 25.41 μM). Finally flow cytometry determined that compound 5d could indeed inhibit the proliferation of HepG2 cells via inducing apoptosis.
Keywords:Tetrandrine  Fangchinoline  Anti-tumor activity  Apoptosis  ZMXPGOXQRSJNCF-LQJZCPKCSA-N  RHUTUXYDKWWVOV-WHNUPTRFSA-N  MZJHEYCWSAFUII-XBZNJEFASA-M  AKJXACZWZCPVOO-HHKZEDCYSA-M  OXBBPSSLCGKDOX-ZUMGYCRCSA-L  WYDZPQBMDZCTMT-VMSJMNQRSA-N  VNBSKOLSTYLJBG-CONSDPRKSA-N  BWAFJYRTDWVKOE-ACHIHNKUSA-N  DYDBAQBYDJCRNC-LQJZCPKCSA-N  FYNLCYYUUNWMRZ-ZPGRZCPFSA-N  ATXYOEZGCUAWRI-CONSDPRKSA-N  MTHFINDLKPTYDJ-KYJUHHDHSA-N  BUUOYVAGXISPLK-ZPQRHCBNSA-N  JAUOQNWDNUNCSN-NSKZCHCTSA-N  QHIZVNHVLKMCBJ-PXLJZGITSA-N  VGJNPLSMROUKSR-CICJRXPUSA-N  SZVMIFUWHSPKNO-ZPGRZCPFSA-N  LGDCEKAFJGBWCH-BCRBLDSWSA-N  BAXSENTVMNHANB-PXLJZGITSA-N  YAXHNBNPQOWVEU-PXLJZGITSA-N  KLESNFABNZWEPY-PXLJZGITSA-N  ZLEYADANFRUNFQ-PXLJZGITSA-N  SNFLUYQPBQAGIO-PXLJZGITSA-N  YLBINMVJGDHYBM-PXLJZGITSA-N  GWZZTCGYHVVXFP-HEVIKAOCSA-N
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