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Updated: Dec 16, 2025

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
Published on: March 6, 2019
Synthesis, antitumor activity, and molecular docking of (-)-epigallocatechin-3-gallate-4β-triazolopodophyllotoxin
Cheng-Ting Zi1,2, Liu Yang3, Yue Hu1
1Key Laboratory of Pu-er Tea Science, Ministry of Education, Yunnan Agricultural University, Kunming 650201, China.
Abstract:
Two new (-)-epigallocatechin-3-gallate-4β-triazolopodophyllotoxin conjugates (7 and 8) were synthesized and evaluated for biological activity. Compound 8 showed highly potent anticancer activity against A-549 cell line with IC50 of 2.16 ± 1.02 μM, which displayed the highest selectivity index value (SI = 14.5) in A-549 cells. Molecular docking indicated that compound 8 could bind with the active site of Top-II. Therefore, compound 8 might be a promising candidate for further development.
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