Synthesis, Antitumor Activity, and Docking Study of 1,3-Disubstituted Imidazolium Derivatives
- Autores: Fan Q.1, Zhong Q.1, Yan H.1
-
Afiliações:
- College of Life Science and Bioengineering
- Edição: Volume 87, Nº 12 (2017)
- Páginas: 3023-3028
- Seção: Letters to the Editor
- URL: https://journals.rcsi.science/1070-3632/article/view/221838
- DOI: https://doi.org/10.1134/S1070363217120489
- ID: 221838
Citar
Resumo
A series of 1,3-disubstituted imidazolium salts were synthesized through a convenient synthetic approach based on the reaction of 1,4-diazabuta-1,3-dienes with HClO4. Their antitumor activity was evaluated in vitro against a number of human cancer cells. 1,3-Bis[(3,5-bis(trifluoromethyl)phenyl]imidazolium perchlorate turned out to be the most active against A549 and MCF-7 cancer cell lines with IC50 values of 5.24 and 4.21 μM, respectively. The results of structure–activity relationship study indicated that substituents on the imidazole derivatives play an important role in their cytotoxic activities. Finally, molecular docking of some tested compounds was carried out in order to investigate their binding pattern with the CDK2.
Palavras-chave
Sobre autores
Q. Fan
College of Life Science and Bioengineering
Email: hongyan@bjut.edu.cn
República Popular da China, Beijing, 100124
Q. Zhong
College of Life Science and Bioengineering
Email: hongyan@bjut.edu.cn
República Popular da China, Beijing, 100124
H. Yan
College of Life Science and Bioengineering
Autor responsável pela correspondência
Email: hongyan@bjut.edu.cn
República Popular da China, Beijing, 100124