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

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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 Hu

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.

Funding

This work was financially supported by Yunnan provincial science and technology department (2015HB093 and 2015FB168) and the National Key Research and Development Program of China (2017YFD0201402).

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