Synthesis of the enantiomers of the bioreductively-activated cytotoxin RSU-1069 and its prodrug RB6145 and lack of stereoselectivity in their cytotoxicity and radiosensitization in vitro.
The R(+)- and S(-)-enantiomers of the radiosensitizer and bioreductively-activated cytotoxin RSU-1069 and their prodrugs have been synthesised. The parent drugs were evaluated as radiosensitizers and bioreductively-activated cytotoxins in vitro. No stereoselectivity in the activities in vitro of the two enantiomers was evident and both compounds were potent hypoxia-selective agents.
Naylor
M A
MA
MRC Radiobiology Unit, Didcot, Oxon, U.K.
Threadgill
M D
MD
Showalter
H D
HD
Stratford
I J
IJ
Stephens
M A
MA
Fielden
E M
EM
Adams
G E
GE
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry; D008920:Misonidazole / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D009593:Nitroimidazoles / Q000138:chemical synthesis* / Q000737:chemistry; D011355:Prodrugs / Q000138:chemical synthesis* / Q000737:chemistry; D011838:Radiation-Sensitizing Agents / Q000138:chemical synthesis* / Q000737:chemistry; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000970:Antineoplastic Agents; D009593:Nitroimidazoles; D011355:Prodrugs; D011838:Radiation-Sensitizing Agents; C067834:RB 6145; C041712:1-(2-nitro-1-imidazolyl)-3-aziridino-2-propanol; D008920:Misonidazole