%0 Journal Article %A Zi, Cheng-Ting %A Yang, Liu %A Dong, Fa-Wu %A Kong, Qing-Hua %A Ding, Zhong-Tao %A Zhou, Jun %A Jiang, Zi-Hua %A Hu, Jiang-Miao %D 2019 %T Synthesis and antitumor activity of camptothecin-4β-triazolopodophyllotoxin conjugates %U https://tandf.figshare.com/articles/journal_contribution/Synthesis_and_antitumor_activity_of_camptothecin-4_-triazolopodophyllotoxin_conjugates/7581467 %R 10.6084/m9.figshare.7581467.v1 %2 https://tandf.figshare.com/ndownloader/files/14079758 %K antitumor activity %K CuAAC reaction %K camptothecin %K podophyllotixin %X

Two 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.

%I Taylor & Francis