Co-reporter:Tao Meng, Wei Wang, Zhixiang Zhang, Lanping Ma, Yongliang Zhang, Zehong Miao, Jingkang Shen
Bioorganic & Medicinal Chemistry 2014 Volume 22(Issue 2) pp:848-855
Publication Date(Web):15 January 2014
DOI:10.1016/j.bmc.2013.12.004
A series of 6H-pyrido[2′,1′:2,3]imidazo[4,5-c]isoquinolin-5(6H)-ones have been synthesized and evaluated for their antiproliferative activities. Among them, compounds 2j and 4d displayed potent cytotoxic activities in vitro against HeLa cell line with IC50 values of 0.07 and 0.06 μM, respectively. In general, the antiproliferative activities are correlated with the inhibitory effect on tubulin polymerization and binding property of the colchicine binding site. In addition, flow cytometry and immunofluorescence analysis revealed selected compounds caused G2/M phase arrest of the cell cycle and disruption of the mitotic spindle assembly, which had correlation with proliferation inhibitory activity.
Co-reporter:Danqi Chen, Aijun Shen, Guanghua Fang, Hongchun Liu, Minmin Zhang, Shuai Tang, Bing Xiong, Lanping Ma, Meiyu Geng, Jingkang Shen
Acta Pharmaceutica Sinica B (January 2016) Volume 6(Issue 1) pp:93-99
Publication Date(Web):January 2016
DOI:10.1016/j.apsb.2015.11.002
