Structure activity studies of a novel cytotoxic benzodiazepine.
Analogues of Bz-423, a pro-apoptotic 1,4-benzodiazepine with potent activity in animal models of systemic lupus erythematosus and rheumatoid arthritis, have been designed, synthesized, and evaluated in cell-culture assays. The results of these experiments have defined the structural elements of this new cytotoxic agent required for activity.
Boitano
Anthony
A
Department of Chemistry, University of Michigan, 930 North University Avenue, Ann Arbor, MI 48109-1055, USA.
Emal
Cory D
CD
Leonetti
Francesco
F
Blatt
Neal B
NB
Dineen
Thomas A
TA
Ellman
Jonathan A
JA
Roush
William R
WR
Opipari
Anthony W
AW
Glick
Gary D
GD
D000818:Animals; D001168:Arthritis / Q000188:drug therapy; D001569:Benzodiazepines / Q000737:chemistry* / Q000633:toxicity*; D016923:Cell Death / Q000187:drug effects / Q000502:physiology; D008177:Lupus Vulgaris / Q000188:drug therapy; D013329:Structure-Activity Relationship
D001569:Benzodiazepines; C468549:Bz-423