title: 2,4-Dihydroxychalcone derivatives as novel potent cell division cycle 25B phosphatase inhibitors and protein tyrosine phosphatase 1B inhibitors.
abstract: Eleven 2,4-dihydroxychalcone compounds were synthesized and identified as reversible and competitive cell division cycle 25 (CDC25) B and protein tyrosine phosphatase (PTP) 1B inhibitors with inhibition values in the micromolar range. The results showed that nine compounds significantly inhibited CDC25B phosphatase, whereas seven compounds inhibited the activity against PTP1B in vitro. Compound 8 had the greatest inhibition activity against CDC25B and PTP1B in vitro, with percentage inhibition values of 97.5% and 96.3% at a dose of 20 microg/mL, respectively. Cytotoxic activity assays revealed that compound 8 was the most potent against HCT116, HeLa, and A549 cells. Furthermore, compound 8 exhibited potent antitumor activity in a colo205 xenograft model.
authors.forename: Chao
authors.initials: C
authors.lastname: Xie
authors.forename: Yuan
authors.initials: Y
authors.lastname: Sun
authors.forename: Cheng-Yan
authors.initials: CY
authors.lastname: Pan
authors.forename: Li-Ming
authors.initials: LM
authors.lastname: Tang
authors.forename: Li-Ping
authors.initials: LP
authors.lastname: Guan
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D047188:Chalcones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004396:Coloring Agents; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D007202:Indicators and Reagents; D051379:Mice; D008807:Mice, Inbred BALB C; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013778:Tetrazolium Salts; D013844:Thiazoles; D020687:cdc25 Phosphatases / Q000037:antagonists & inhibitors*
chemical_list: D000970:Antineoplastic Agents; D047188:Chalcones; D004396:Coloring Agents; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D013778:Tetrazolium Salts; D013844:Thiazoles; C059354:2',4'-dihydroxychalcone; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D020687:cdc25 Phosphatases; C022616:thiazolyl blue