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Rapid assembly of 1,3-indanedione-based spirocyclic tetrahydroquinolines for inducing human lung cancer cell apoptosis

查看全文 作　　者：Fen [1,2]Tan;Luojia [1,3]Chen;Yuncong [1,3]Yuan;Xiaoyu [1,3]He;Yiwen [1,3]Su;Shuqiang [1,3]Cao;Conghua [1,4]Xie;Meijia [1,3]Gu;Youquan [1,3,5]Zou 高影响力作者 机构地区：[1]Department of Radiation and Medical Oncology,Zhongnan Hospital of Wuhan University,School of Pharmaceutical Sciences,Wuhan University,Wuhan 430071,China;[2]Hubei Key Laboratory of Purification and Application of Plant Anti-cancer Active Ingredients,Hubei University of Education,Wuhan 430205,China;[3]Key Laboratory of Combinatorial Biosynthesis and Drug Discovery,Ministry of Education,Wuhan University,Wuhan 430071,China;[4]Hubei Key Laboratory of Tumor Biological Behaviors,Hubei Cancer Clinical Study Center,Zhongnan Hospital of Wuhan University,Wuhan 430071,China;[5]TaiKang Center for Life and Medical Sciences,Wuhan University,Wuhan 430071,China高影响力机构 出　　处：《Green Synthesis and Catalysis》索引2022年第3卷第4期,共16页高影响力期刊 基　　金：Financial support from the National Natural Science Foundation of China(No.21602052);the start-up funding from Wuhan University(Nos.691000002 and 600460026)are gratefully acknowledged.The authors thank Prof.Dr.Xianggao Meng(Central China Normal University)for performing the X-ray crystal analysis. 摘　　要：The rapid collection of a library of biologically relevant molecules is essential in new drug discovery.Here we show a variety of bioactive 1,3-indanedione-based spirocyclic tetrahydroquinolines that have been concisely and efficiently constructed under the guidance of biology-oriented synthesis(BIOS).Using Pd(PPh_(3))_(4) as a catalyst,various 2-arylidene-1,3-indanediones can react with vinyl benzoxazinanones under the mild condition to afford a new class of spirocyclic tetrahydroquinolines in moderate to excellent yields(45%-99%)with high stereocontrol(>95:5 diastereoselectivity).Their structures were unambiguously confirmed by X-ray single crystal analysis.The biological evaluation revealed that two of the 1,3-indanedione-based spirocyclic tetrahydroquinolines show remarkable apoptosis-inducing activities over A549 human lung cancer cells,exceeding that of cisplatin.The antitur activities were triggered by reactive oxygen species,commonly overproduced in cancer cells.The clinical demand for antitumor chemotherapy for lung cancer has encouraged an all-out search for analogues with lower toxcity,improved therapeutic index and increased activity. 关 键 词：Spirocyclic tetrahydroquinoline 1,3-Indanedione Lung cancer Apoptosis MITOCHONDRIA
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