Chloro-oxime derivatives as novel small molecule chaperone amplifiers

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 11, 2009, Pages 3128-3135

  Zhou, Yuefen ^a   Vu, Khang ^a   Chen, Yongsheng ^a   Pham, John ^a   Brady, Thomas ^a   Liu, Gang ^a   Chen, Jinhua ^a   Nam, Joonwoo ^a   Murali Mohan Reddy, P S ^a   Au, Qingyan ^a   Yoon, Il Sang ^a   Tremblay, Marie Helene ^a   Yip, Gary ^a   Cher, Charmian ^a   Zhang, Bin ^a   Barber, Jack R ^a   Ng, Shi Chung ^a  

^a CytRx Corporation   (United States)

Author keywords

Chloro oxime derivatives; Cytoprotection; ER stress; HSF1, heat shock proteins (HSPs); MG 132 stress; Neurodegenerative diseases; PolyQ stress; Protein misfolding; Small molecule chaperone amplifiers; Stress granule

Indexed keywords

BENZYLOXYCARBONYLLEUCYLLEUCYLLEUCINAL; CHAPERONE; CHLORO OXIME DERIVATIVE; HEAT SHOCK TRANSCRIPTION FACTOR 1; LEAD; OXIME DERIVATIVE; UNCLASSIFIED DRUG;

AMPLIFIER; ARTICLE; CELL PROTECTION; CYTOTOXICITY; DRUG SYNTHESIS; ENDOPLASMIC RETICULUM STRESS; FEMALE; HUMAN; HUMAN CELL; STRUCTURE ACTIVITY RELATION; TRANSCRIPTION INITIATION;

CELL LINE, TUMOR; CYTOPROTECTION; DNA-BINDING PROTEINS; HUMANS; MOLECULAR CHAPERONES; OXIMES; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSCRIPTION FACTORS;

EID: 65149106747     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.03.011     Document Type: Article

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23. 50 value is the concentration at which 50% of cells have positive granule formation. The average standard deviation for the data in Tables 2 and 3 generated from this assay was 34% for multiple testing of same compounds in different runs.
24. 50 value is the concentration at which the cell numbers increase 50% by comparing with MG-132 treatment alone without compound. The compounds were tested in the concentration range of 0.3-80 μM with twofold dilution and the maximum percentage of the cytoprotection >60% is considered active. The average standard deviation for the data in Tables 2 and 3 generated from this assay was 26% for multiple testing of same compounds in different runs.
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26. 50 values and curve fitting were calculated using prism 4.0 (graphpad Software, San Diego, CA) with nonlinear regression analysis. The average standard deviation for the data in Tables 2 and 3 generated from MTS_Hela and MTS_SK assays were 34% and 14%, respectively, for multiple testing of same compounds in different runs.
27. 50 values and curve fitting were calculated using prism 4.0 (graphpad Software, San Diego, CA) with nonlinear regression analysis.
28. polyQ alone × 100 (%).