Design, synthesis, and evaluation of bromo-retrochalcone derivatives as protein tyrosine phosphatase 1B inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 12, 2011, Pages 3755-3758

  Liu, Zhiguo ^a   Lee, Woojung ^b   Kim, Su Nam ^b   Yoon, Goo ^c   Cheon, Seung Hoon ^a  

^a Chonnam National University   (South Korea)

^b Korea Institute of Science and Technology   (South Korea)

^c Mokpo National University   (South Korea)

Author keywords

Bromo retrochalcone; Licochalcone; Protein tyrosine phosphatase 1B; Synthetic

Indexed keywords

BROMO RETROCHALCONE DERIVATIVE; LICOCHALCONE A; LICOCHALCONE E; PROTEIN TYROSINE PHOSPHATASE 1B INHIBITOR; UNCLASSIFIED DRUG; URSOLIC ACID;

ARTICLE; DRUG ACTIVITY; DRUG DESIGN; DRUG INHIBITION; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; IC 50;

BROMINE; CHALCONES; DRUG DESIGN; ENZYME ACTIVATION; INHIBITORY CONCENTRATION 50; MOLECULAR STRUCTURE; PROTEIN TYROSINE PHOSPHATASE, NON-RECEPTOR TYPE 1; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79957812480     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.04.057     Document Type: Article

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10. PTP1B assay: Recombinant human PTP1B was purchased from BIOMOL International LP. For the inhibition assay, a sample (3 μL in DMSO) was added to a reaction mixture containing enzyme (2 μL), reaction buffer [10 μL, 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol], water (35 μL) and 50 μL of 4mM p-nitrophenyl phosphate (pNPP). The reaction mixture (100 μL) was incubated at 37 °C for 30 min and then quenched by addition of 10 μL of 10 N NaOH. The hydrolysis of pNPP was determined by measuring the absorbance at 405 nm.