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

Title
Chalcones, inhibitors for topoisomerase i and cathepsin B and L, as potential anti-cancer agents
Authors
Kim S.-H.Lee E.Baek K.H.Kwon H.B.Woo H.Lee E.-S.Kwon Y.Na Y.
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2013
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894XJCR Link
Citation
vol. 23, no. 11, pp. 3320 - 3324
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
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. © 2013 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2013.03.106
Appears in Collections:
약학대학 > 약학과 > Journal papers
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