Chalcones, inhibitors for topoisomerase i and cathepsin B and L, as potential anti-cancer agents

Seok Ho Kim, Eunyoung Lee, Kyung Hye Baek, Han Byeol Kwon, Hyunjung Woo, Eung Seok Lee, Youngjoo Kwon, Younghwa Na

Research output: Contribution to journalArticlepeer-review

45 Scopus citations


In order to diversify the pharmacological activity of chalcones and extend the scaffold of topoisomerase and cathepsins B and L inhibitors, we have designed and synthesized total 18 chalcone compounds and tested their biological activity. In the topoisomerase inhibition test, most analogues in group III and IV except compound 11 exhibited more efficient topoisomerase I inhibitory activity than camptothecin at 20 μM. Compounds 15, 16 and 18 in group IV showed significant cathepsin B and L inhibitory activity. Among the compounds, compound 15 was most active with IC50 values of 1.81 ± 0.05 μM on cathepsin B and 3.15 ± 0.07 μM on cathepsin L, respectively. Compound 15 also showed most potent cytotoxic activity against T47D and SNU638 cells with IC50 values of 1.37 ± 0.05 μM and 0.62 ± 0.01 μM, respectively. Overall, although more compounds should be tested and analyzed for clear SAR against topoisomerase I and cathepsin B and L, compound 15 showed consistent inhibitory ability on the tested assays, which can implicate the cytotoxic activity of compound 15 on topoisomerase I and cathepsin B and L inhibitory pathways.

Original languageEnglish
Pages (from-to)3320-3324
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number11
StatePublished - 1 Jun 2013

Bibliographical note

Funding Information:
This work was financially supported by CHA University, Pocheon, Korea.


  • Cathepsin Band L
  • Chalcone
  • Cytotoxicity
  • Topoisomerase I


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