Design, synthesis and bioevaluation of novel trifluoromethylquinoline derivatives as tubulin polymerization inhibitors

Author:

Zhang Sisi123,Mo Min123,Lv Mengfan124,Xia Wen5,Liu Kun12,Yu Gang12,Yu Jia12,Xu Guangcan12,Zeng Xiaoping12,Cheng Sha12,Xu Bixue12,Luo Heng12,Meng Xueling12ORCID

Affiliation:

1. State Key Laboratory of Functions & Applications of Medicinal Plants, Guizhou Medical University, Guiyang, 550014, China

2. Natural Products Research Center of Guizhou Province, Guiyang, 550014, China

3. School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang, 550025, China

4. Guizhou University of Traditional Chinese Medicine, Guiyang, 550025, PR China

5. Guizhou Bailing Enterprise Group Pharmaceutical Co. Ltd, Anshun Guizhou, 561000, China

Abstract

Aim: A series of novel trifluoromethylquinoline derivatives were designed, synthesized and evaluated for antitumor activities. Methodology: All compounds were evaluated for antiproliferative activity against four human cancer cell lines. Results: Among them, 5a, 5m, 5o and 6b exhibited remarkable antiproliferative activities against all the tested cell lines at nanomolar concentrations. Mechanism of action studies demonstrated that 6b targeted the colchicine binding site, potentially inhibiting tubulin polymerization, and further studies indicated that 6b could arrest LNCaP cells in the G2/M phase and induce cell apoptosis. Molecular docking confirmed that 6b could bind to the colchicine binding site. Conclusion: Results suggested that 6b could serve as a promising lead compound for the development of novel tubulin polymerization inhibitors and cancer therapy.

Funder

Department of Education of Guizhou Province

Science and Technology Department of Guizhou Province

Natural Science Foundations of China

Organisation Board of Guizhou Province

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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