含吲哚骨架衍生物作为微管蛋白抑制剂的研究
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摘要
微管作为细胞骨架的主要成分,在细胞的分裂过程中起着重要的作用,近年来,微管已经成为抗肿瘤药物研发的重要靶点之一。吲哚作为一种含氮的芳香杂环生物碱,因其良好的生物活性,在抗肿瘤药物设计研发领域备受关注,越来越多能够抑制微管蛋白的吲哚类衍生物被相继报道。本文对近年来已经报道的含有吲哚骨架合成或者半合成的抑制剂进行了综述。
As the main component of the cytoskeleton, microtubules play an important role in the process of cell division. In recent years, microtubules have become one of the important targets for the development of anti-tumor drugs. As a nitrogen-containing aromatic heterocyclic alkaloid, indole has attracted much attention in the design and development of anti-tumor drugs due to its good biological activity, more and more indoles derivatives that can inhibit tubulin have been reported successively. In this paper, the synthetic or semi-synthetic inhibitors containing indoles skeletons that have been reported in recent years are reviewed.
As the main component of the cytoskeleton, microtubules play an important role in the process of cell division. In recent years, microtubules have become one of the important targets for the development of anti-tumor drugs. As a nitrogen-containing aromatic heterocyclic alkaloid, indole has attracted much attention in the design and development of anti-tumor drugs due to its good biological activity, more and more indoles derivatives that can inhibit tubulin have been reported successively. In this paper, the synthetic or semi-synthetic inhibitors containing indoles skeletons that have been reported in recent years are reviewed.
引文
[1]张婷玉,叶建仁.抗肿瘤的微管抑制剂的研究进展[J].福建农业,2014(8):171.
[2]杨梦如.吲哚类衍生物作为tubulin抑制剂的设计、合成及生物活性评价[D].南京:南京大学,2016.
[3]Mohan R,Banerjee M,Ray A,et al.Antimitotic Sulfonamides Inhibit Microtubule Assembly Dynamics and Cancer Cell Proliferation[J].Biochemistry,2006,45:5440-5449.
[4]Renukadevi Patil,Siddappa A Patil,Kenneth D Beaman,et al.Indole Molecules as Inhibitors of Tubulin Polymerization:Potential New Anticancer Agents,an Update[J].Future Med.Chem.2016,8(11):1291-1316.
[5]Duan YT,Sang YL,Makawana JA et al.Discovery and Molecular Modeling of Novel 1-Indolyl Acetate-5-Nitroimidazole Targeting Tubulin Polymerization as Antiproliferative Agents[J].Eur.J.Med.Chem,2014,85:341-351.
[6]Kamal A,Rao MP,Das P et al.Synthesis and Biologica Evaluation of Imidazo[2,1-B][1,3,4]Thiadiazole-Linked Oxindoles as Potent Tubulin Polymerization Inhibitors[J].Chem Med Chem,2014,9(7):1463-1475.
[7]Hu MJ,Zhang B,Yang HK et al.Design,Synthesis and Molecular Docking Studies of Novel Indole-Pyrimidine Hybrids as Tubulin Polymerization Inhibitors[J].Chem.Biol.Drug Des.,2015,86(6):1491-1500.
[8]Knaack M,Emig P,Bats JW,et al.Synthesis and characterization of the biologically active 2-[1-(4-chlorobenzyl)-1Hindol-3-yl]-2-oxo-N-pyridin-4-yl acetamide[J].Eur J OrgChem,2001,20:3843-3847.
[9]Baytas SN,Inceler N,Yilmaz A et al.Synthesis,Biological Evaluation and Molecular Docking Studies of Trans-Indole-3-Acrylamide Derivatives,a New Class of Tubulin Polymerization Inhibitors[J].Bioorg.Med.Chem.,2014,22(12):3096-3104.
[10]尚海,潘莉,杨澍,等.微管蛋白抑制剂的研究进展[J].药学学报,2010,45(9):1078-1088.
[11]Li Q,Woods KW,Claiborne A,et al.Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors.Discovery of A-289099 as an orally active antitumor agent[J].Bioorg Med Chem Lett,2002,12:465-469.
[2]杨梦如.吲哚类衍生物作为tubulin抑制剂的设计、合成及生物活性评价[D].南京:南京大学,2016.
[3]Mohan R,Banerjee M,Ray A,et al.Antimitotic Sulfonamides Inhibit Microtubule Assembly Dynamics and Cancer Cell Proliferation[J].Biochemistry,2006,45:5440-5449.
[4]Renukadevi Patil,Siddappa A Patil,Kenneth D Beaman,et al.Indole Molecules as Inhibitors of Tubulin Polymerization:Potential New Anticancer Agents,an Update[J].Future Med.Chem.2016,8(11):1291-1316.
[5]Duan YT,Sang YL,Makawana JA et al.Discovery and Molecular Modeling of Novel 1-Indolyl Acetate-5-Nitroimidazole Targeting Tubulin Polymerization as Antiproliferative Agents[J].Eur.J.Med.Chem,2014,85:341-351.
[6]Kamal A,Rao MP,Das P et al.Synthesis and Biologica Evaluation of Imidazo[2,1-B][1,3,4]Thiadiazole-Linked Oxindoles as Potent Tubulin Polymerization Inhibitors[J].Chem Med Chem,2014,9(7):1463-1475.
[7]Hu MJ,Zhang B,Yang HK et al.Design,Synthesis and Molecular Docking Studies of Novel Indole-Pyrimidine Hybrids as Tubulin Polymerization Inhibitors[J].Chem.Biol.Drug Des.,2015,86(6):1491-1500.
[8]Knaack M,Emig P,Bats JW,et al.Synthesis and characterization of the biologically active 2-[1-(4-chlorobenzyl)-1Hindol-3-yl]-2-oxo-N-pyridin-4-yl acetamide[J].Eur J OrgChem,2001,20:3843-3847.
[9]Baytas SN,Inceler N,Yilmaz A et al.Synthesis,Biological Evaluation and Molecular Docking Studies of Trans-Indole-3-Acrylamide Derivatives,a New Class of Tubulin Polymerization Inhibitors[J].Bioorg.Med.Chem.,2014,22(12):3096-3104.
[10]尚海,潘莉,杨澍,等.微管蛋白抑制剂的研究进展[J].药学学报,2010,45(9):1078-1088.
[11]Li Q,Woods KW,Claiborne A,et al.Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors.Discovery of A-289099 as an orally active antitumor agent[J].Bioorg Med Chem Lett,2002,12:465-469.
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