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Discovery of pyrazole-carbohydrazide with indole moiety as tubulin polymerization inhibitors and anti-tumor candidates

文献类型： 外文期刊

作者： Man, Ruo-Jun 1 ; Lu, Tian 1 ; Zheng, Chi-Chong 1 ; Li, Tong 1 ; Wu, Meng-Ke 1 ; Li, Dong-Dong 3 ; He, Xue-Mei 2 ;

作者机构： 1.Guangxi Minzu Univ, Guangxi Key Lab Polysaccharide Mat & Modificat, Nanning, Peoples R China

2.Guangxi Acad Agr Sci, Agrofood Sci & Technol Res Inst, Nanning, Peoples R China

3.Nanjing Forestry Univ, Coll Chem Engn, Nanjing, Peoples R China

4.Guangxi Key Lab Fruits & Vegetables Storage Proc T, Nanning, Peoples R China

5.Guangxi Minzu Univ, Guangxi Key Lab Polysaccharide Mat & Modificat, Nanning 530008, Peoples R China

6.Nanjing Forestry Univ, Coll Chem Engn, 159 Longpan Rd, Nanjing 210037, Peoples R China

7.Guangxi Acad Agr Sci, Agrofood Sci & Technol Res Inst, 174 EastDaxue Rd, Nanning 530007, Peoples R China

关键词： antitumor candidates; indole moiety; pyrazole-carbohydrazide; tubulin polymerization inhibitor

期刊名称：DRUG DEVELOPMENT RESEARCH （ 影响因子：5.004； 五年影响因子：4.264 ）

ISSN： 0272-4391

年卷期：

页码：

收录情况： SCI

摘要： In this work, a series of indole-containing pyrazole-carbohydrazide derivatives A1-A25 were synthesized, and their biological activity on tubulin polymerization inhibition and mitotic catastrophe was evaluated. For introducing indole group to CA-4 pattern, the carbohydrazide linker was used for the first time. As the top hit, A18 suggested notable antiproliferation efficacy and tubulin polymerization inhibitory activity. Inferring comparable antitubulin effect with the positive control Colchicine, A18 indicated obviously lower cyto-toxicity. The cell scratch test showed that A18 could block the cell migration, while the confocal imaging depicted that A18 could induce the mitotic catastrophe via a Colchicine-like approach. The docking simulation visualized the probable binding pattern of A18. With the information in this work, some new hints on modification might be involved in further tubulin-related investigations.

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