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Design, synthesis and biological evaluation of novel indole-based oxalamide and aminoacetamide derivatives as tubulin polymerization inhibitors. 2020

Peng-Cheng Diao, and Xie-Er Jian, and Peng Chen, and Chuan Huang, and Jie Yin, and Jie Chun Huang, and Jun-Sheng Li, and Pei-Liang Zhao
Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Science, Southern Medical University, Guangzhou 510515, PR China.

A series of novel indole-based oxalamide and aminoacetamide derivatives were designed, synthesized, and evaluated for antiproliferative activities. Preliminary results revealed that compound 8g exhibited significant antiproliferative effect against PC-3, HeLa and HCT-116 cell lines. Flow cytometric analysis of the cell cycle demonstrated the compound 8g induced the cell cycle arrest at G2/M phase in HeLa cell lines. Immunocytochemistry revealed loss of intact microtubule structure in cells treated with 8g andinhibition of tubulinpolymerization. Additionally, molecular docking analysis suggested that 8g formed stable interactions in the colchicine-binding site of tubulin. These preliminary results demonstrated that a new class of novel indole-based oxalamide and aminoacetamide derivatives described in the investigation could be developed as potential scaffolds to new anticancer agents.

UI MeSH Term Description Entries
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular
D050257 Tubulin Modulators Agents that interact with TUBULIN to inhibit or promote polymerization of MICROTUBULES. Microtubule Modulator,Tubulin Inhibitor,Tubulin Modulator,Tubulin Polymerization Inhibitor,Tubulin Polymerization Promoter,Tubulin Promoter,Microtubule Modulators,Tubulin Inhibitors,Tubulin Polymerization Inhibitors,Tubulin Polymerization Promoters,Tubulin Promoters,Inhibitor, Tubulin,Inhibitor, Tubulin Polymerization,Inhibitors, Tubulin,Inhibitors, Tubulin Polymerization,Modulator, Microtubule,Modulator, Tubulin,Modulators, Microtubule,Modulators, Tubulin,Polymerization Inhibitor, Tubulin,Polymerization Inhibitors, Tubulin,Polymerization Promoter, Tubulin,Polymerization Promoters, Tubulin,Promoter, Tubulin,Promoter, Tubulin Polymerization,Promoters, Tubulin,Promoters, Tubulin Polymerization

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