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Chalcones derivatives as potent Cell division cycle 25B phosphatase inhibitors
- Source :
- Pharmacological Reports; May 2014, Vol. 66 Issue: 3 p515-519, 5p
- Publication Year :
- 2014
-
Abstract
- To discover novel cell division cycle 25 (CDC25) B inhibitors and elucidate the mechanisms of inhibition in cancer cells. Nineteen 2'-hydroxy-4'-isoprenyloxychalcone derivatives (a-s) were evaluated the inhibition CDC25B activity. The enzymatic activities of the CDC25B catalytic domain were determined by monitoring the dephosphorylation of OMFP. Cell growth inhibition was detected by MTT assay. The results showed that sixteen compounds significantly inhibited cycle 25B phosphatase in vitro. Among, three compounds k, rand shad the best inhibition activity and significantly inhibited CDC25B with inhibition rates against CDC25B of 99.95%, 99.75%, and 97.77%, respectively, which is similar to the reference drugs Na3VO4(98%). Cytotoxic activity assays showed compounds kand rare the potent against HCT116, HeLa, and A549 cells, moreover, compound kdelayed the potent tumor inhibitory activity in a colo205 xenograft model in vivo.
Details
- Language :
- English
- ISSN :
- 17341140 and 22995684
- Volume :
- 66
- Issue :
- 3
- Database :
- Supplemental Index
- Journal :
- Pharmacological Reports
- Publication Type :
- Periodical
- Accession number :
- ejs52298347
- Full Text :
- https://doi.org/10.1016/j.pharep.2013.08.016