Synthesis and antitumor activity of camptothecin-4β-triazolopodophyllotoxin conjugates

<p>Two new compounds (<b>9</b> and <b>10</b>) 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 <b>10</b> showed highly potent against HL-60 cell line tested, with IC<sub>50</sub> value 17.69 ± 0.19 μM. This compound suggested its potential as anticancer agents for further development.</p>