Molecular diversity of trimethoxyphenyl-1,2,3-triazole hybrids as novel colchicine site tubulin polymerization inhibitors
Molecular diversity of trimethoxyphenyl-1,2,3-triazole hybrids as novel colchicine site tubulin polymerization inhibitors
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作为新型秋水仙碱位点微管蛋白聚合抑制剂的三甲氧基苯基-1,2,3-三唑杂化物的分子多样性
DOI：
10.1016/j.ejmech.2019.01.033
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发表时间：
2019-03-01
影响因子：
6.7
通讯作者：
Zhang, Sai-Yang
中科院分区：
文献类型：
--
作者：
Fu, Dong-Jun;Li, Ping;Zhang, Sai-Yang
设计、合成了结构多样的三甲氧基苯基-1，2，3-三唑杂合物，并评价了它们对三种癌细胞系（PC 3、MGC 803和HepG 2）的抗增殖活性。其中，含有香豆素片段19 c的三甲氧基苯基-1，2，3-三唑显示出比抗癌药物秋水仙碱更好的抗增殖活性结果，IC 50值为0.13 μ M至1.74 μ M。化合物19 c可抑制MGC 803细胞生长和集落形成，通过下调CDK 1的表达诱导细胞周期阻滞于G2/M期，通过调节DRS和Bcl-2家族的表达促进细胞凋亡。此外，19 c强烈抑制微管蛋白聚合的相互作用与秋水仙碱网站。(C)2019 Elsevier Masson SAS。All rights reserved.
Structurally diverse trimethoxyphenyl-1,2,3-triazole hybrids were designed, synthesized and evaluated for their antiproliferative activity against three cancer cell lines (PC3, MGC803 and HepG2). Among them, trimethoxyphenyl-1,2,3-triazole containing the coumarin fragement 19c displayed better anti proliferative activity results with IC50 values from 0.13 mu M to 1.74 mu M than anticancer drug colchicine. Compound 19c could inhibit MGC803 cell growth and colony formation, induce G2/M phase arrest by down expression of CDK1, and promote apoptosis by regulating DRS and Bcl-2 family. Moreover, 19c strongly inhibited tubulin polymerization by interacting with the colchicine site. (C) 2019 Elsevier Masson SAS. All rights reserved.