gnpl_a_1538223_sm4508.pdf (1.16 MB)
Synthesis and antitumor activity of camptothecin-4β-triazolopodophyllotoxin conjugates
journal contribution
posted on 2019-01-12, 09:27 authored by Cheng-Ting Zi, Liu Yang, Fa-Wu Dong, Qing-Hua Kong, Zhong-Tao Ding, Jun Zhou, Zi-Hua Jiang, Jiang-Miao HuTwo new compounds (9 and 10) having a camptothecin (CPT) analog conjugated to the 4β-azido-4-deoxypodophyllotixin analog by untilizing the copper-catalyzed azide-alkyne cycloadditon (CuAAC) reaction, and were evaluated for their cytotoxicity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using the MTT (3-(4,5-dimethyl-thiahiazo-2-yl)-2,5-diphenyltetrazolium bromide) assay. Two novel conjugates shown weak cytotoxicity, compound 10 showed highly potent against HL-60 cell line tested, with IC50 value 17.69 ± 0.19 μM. This compound suggested its potential as anticancer agents for further development.