Chloro-oxime derivatives as novel small molecule chaperone amplifiers.
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).
Zhou
Yuefen
Y
CytRx Corporation, San Diego, CA 92109, USA. yuefen.zhou@gmail.com
Vu
Khang
K
Chen
Yongsheng
Y
Pham
John
J
Brady
Thomas
T
Liu
Gang
G
Chen
Jinhua
J
Nam
Joonwoo
J
Murali Mohan Reddy
P S
PS
Au
Qingyan
Q
Yoon
Il Sang
IS
Tremblay
Marie-Helene
MH
Yip
Gary
G
Cher
Charmian
C
Zhang
Bin
B
Barber
Jack R
JR
Ng
Shi Chung
SC
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
D004268:DNA-Binding Proteins; C000619706:HSF1 protein, human; D000076249:Heat Shock Transcription Factors; D018832:Molecular Chaperones; D010091:Oximes; D014157:Transcription Factors