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Chalcones derivatives as potent Cell division cycle 25B phosphatase inhibitors
- Source :
- Pharmacological Reports. 66:515-519
- Publication Year :
- 2014
- Publisher :
- Springer Science and Business Media LLC, 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, r and s had 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 k and r are the potent against HCT116, HeLa, and A549 cells, moreover, compound k delayed the potent tumor inhibitory activity in a colo205 xenograft model in vivo.
- Subjects :
- Male
Cdc25
Phosphatase
Mice, Nude
Antineoplastic Agents
Biology
Dephosphorylation
HeLa
Mice
Chalcones
Tumor Cells, Cultured
Animals
Humans
cdc25 Phosphatases
MTT assay
Enzyme Inhibitors
Pharmacology
A549 cell
Mice, Inbred BALB C
Cell growth
Cell Cycle
General Medicine
HCT116 Cells
biology.organism_classification
Molecular biology
Biochemistry
Cancer cell
biology.protein
HeLa Cells
Subjects
Details
- ISSN :
- 17341140
- Volume :
- 66
- Database :
- OpenAIRE
- Journal :
- Pharmacological Reports
- Accession number :
- edsair.doi.dedup.....be8f174f5881451703aa6f5663d3a9c8