Design, synthesis and biological activities of tetrandrine and fangchinoline derivatives as antitumer agents. Issue 3 (1st February 2017)

• Record Type: Journal Article
• Authors: Li, Dechao; Liu, Haizheng; Liu, Yufa; Zhang, Qikun; Liu, Chao; Zhao, Shuhua; Jiao, Bo
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 3(2017)
• Page Start: 533
• Page End: 536
• Publication Date: 2017-02-01
• Subjects: 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; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.12.029
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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 (compound5d ) exhibited the most significant cytotoxic effects. Compound5d 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 compound5d could indeed inhibit the proliferation of HepG2 cells via inducing apoptosis.