Amide derivatives of ethacrynic acid: Synthesis and evaluation as antagonists of Wnt/β-catenin signaling and CLL cell survival

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 3, 2009, Pages 606-609

  Jin, Guangyi ^a   Lu, Desheng ^a   Yao, Shiyin ^a   Wu, Christina C N ^a   Liu, Jerry X ^a   Carson, Dennis A ^a   Cottam, Howard B ^a  

^a UNIVERSITY OF CALIFORNIA SAN DIEGO   (United States)

Author keywords

Chronic lymphocytic leukemia; Ethacrynic acid amides; Lef 1; Wnt catenin signaling

Indexed keywords

AMIDE; BETA CATENIN; ETACRYNIC ACID; THIOL DERIVATIVE; TRANSCRIPTION FACTOR; WNT PROTEIN;

ARTICLE; CELL SURVIVAL; CHEMICAL BOND; COVALENT BOND; DRUG MECHANISM; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; HUMAN; HUMAN CELL; LEUKEMIA CELL; REDUCTION; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION;

ANTINEOPLASTIC AGENTS; BETA CATENIN; CARBON; CELL LINE, TUMOR; CELL SURVIVAL; CHEMISTRY, PHARMACEUTICAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; DRUG SCREENING ASSAYS, ANTITUMOR; ETHACRYNIC ACID; HUMANS; INHIBITORY CONCENTRATION 50; MODELS, CHEMICAL; SIGNAL TRANSDUCTION; WNT PROTEINS;

EID: 58549110011     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.12.067     Document Type: Article

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16. 6 They included the β-catenin regulated TOPFlash reporter gene and expression plasmids for Wnt1, Wnt3, β-catenin, DSH, LRP6, as described.
17. 50 determined using Prism 4.0a software (GraphPad).
18. 5 per well and treated with compounds for 48 h. Then 1/10 V of 5 mg/mL MTT was added, and cells were incubated at 37 °C overnight. Finally, 1/2 V of Lysis buffer was added to dissolve the insoluble purple formazan product, incubated at 37 °C overnight, and OD at 570 nm was read and recorded.
19. 4, and the residue was purified by silica gel column chromatography (dichloromethane:methanol from 100:0 to 100:5) to obtain the pure EA amides shown in Table 1.
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