title: Chloro-oxime derivatives as novel small molecule chaperone amplifiers.
abstract: Chloro-oxime derivatives were investigated as novel small molecule chaperone amplifiers. Lead optimization led to the discovery of compounds that displayed potent HSF1 activation activity, significant cytoprotection in MG-132 stress, ER stress and PolyQ stress cell models (EC(50)<10 microM).
authors.affiliation: CytRx Corporation, San Diego, CA 92109, USA. yuefen.zhou@gmail.com
authors.forename: Yuefen
authors.initials: Y
authors.lastname: Zhou
authors.forename: Khang
authors.initials: K
authors.lastname: Vu
authors.forename: Yongsheng
authors.initials: Y
authors.lastname: Chen
authors.forename: John
authors.initials: J
authors.lastname: Pham
authors.forename: Thomas
authors.initials: T
authors.lastname: Brady
authors.forename: Gang
authors.initials: G
authors.lastname: Liu
authors.forename: Jinhua
authors.initials: J
authors.lastname: Chen
authors.forename: Joonwoo
authors.initials: J
authors.lastname: Nam
authors.forename: P S
authors.initials: PS
authors.lastname: Murali Mohan Reddy
authors.forename: Qingyan
authors.initials: Q
authors.lastname: Au
authors.forename: Il Sang
authors.initials: IS
authors.lastname: Yoon
authors.forename: Marie-Helene
authors.initials: MH
authors.lastname: Tremblay
authors.forename: Gary
authors.initials: G
authors.lastname: Yip
authors.forename: Charmian
authors.initials: C
authors.lastname: Cher
authors.forename: Bin
authors.initials: B
authors.lastname: Zhang
authors.forename: Jack R
authors.initials: JR
authors.lastname: Barber
authors.forename: Shi Chung
authors.initials: SC
authors.lastname: Ng
mesh_terms: D045744:Cell Line, Tumor; D019610:Cytoprotection; D004268:DNA-Binding Proteins / Q000378:metabolism; D000076249:Heat Shock Transcription Factors; D006801:Humans; D018832:Molecular Chaperones / Q000737:chemistry* / Q000378:metabolism; D010091:Oximes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014157:Transcription Factors / Q000378:metabolism
chemical_list: D004268:DNA-Binding Proteins; C000619706:HSF1 protein, human; D000076249:Heat Shock Transcription Factors; D018832:Molecular Chaperones; D010091:Oximes; D014157:Transcription Factors