4.4 Article

Synthesis, antitumor activity, and molecular docking of (-)-epigallocatechin-3-gallate-4β-triazolopodophyllotoxin conjugates

Journal

JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
Volume 23, Issue 8, Pages 772-780

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/10286020.2020.1786066

Keywords

Podophyllotixin; EGCG; click reaction; antitumor activity; molecular docking

Funding

  1. National Nature Science Foundation of China [21602196, 31960075]
  2. Science and Technology Project of Yunnan province [2017ZF003, 2017FD084, 2017FG001-046]
  3. Yunnan Agricultural University Natural Science Foundation for Young Scientists and Postgraduates [2015ZR08]

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Two new (-)-epigallocatechin-3-gallate-4 beta-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 the highest selectivity index value (SI = 14.5) in A-549 cells, indicating its potential as a promising candidate for further development.
Two new (-)-epigallocatechin-3-gallate-4 beta-triazolopodophyllotoxin conjugates (7and8) were synthesized and evaluated for biological activity. Compound8showed highly potent anticancer activity against A-549 cell line with IC(50)of 2.16 +/- 1.02 mu M, which displayed the highest selectivity index value (SI = 14.5) in A-549 cells. Molecular docking indicated that compound8could bind with the active site of Top-II. Therefore, compound8might be a promising candidate for further development.

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