Synthesis and biological evaluation of 1,2,5-oxadiazole N-oxide derivatives as hypoxia-selective cytotoxins.
Synthesis and biological evaluation of new 1,2,5-oxadiazole N-oxide derivatives with potential cytotoxic effects are described. From the series of compounds tested, compounds 2 and 6 proved to be very active, although non-selective.
Monge
A
A
Department of Medicinal Chemistry, University of Navarra, Pamplona, Spain.
López de Ceráin
A
A
Ezpeleta
O
O
Cerecetto
H
H
Dias
E
E
Di Maio
R
R
González
M
M
Onetto
S
S
Seoane
G
G
Suescun
L
L
Mariezcurrena
R
R
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015687:Cell Hypoxia / Q000187:drug effects; D006224:Cricetinae; D003412:Cricetulus; D003497:Cyclic N-Oxides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D008958:Models, Molecular; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014407:Tumor Cells, Cultured; D014961:X-Ray Diffraction
C116849:3-chloromethyl-4-phenyl-1,2,5-oxadiazole-2-oxide; C116850:4-phenyl-1,2,5-oxadiazole-3-carboxaldehyde-2-oxide; D000970:Antineoplastic Agents; D003497:Cyclic N-Oxides; D010069:Oxadiazoles