Synthesis, chemical stability and pre-clinical anti-tumor activity of pyrazine diazohydroxide, sodium salt (NSC-361456).
The synthesis, chemical stability and anti-tumor activity of pyrazine diazohydroxide, sodium salt, a compound that has been selected for development to clinical trials, are described. The compound shows a half-life of about 100 minutes at pH 7.4 and is active against a number of experimental tumors.
Baker
D C
DC
Department of Chemistry, University of Alabama, Tuscaloosa 35487-9671.
Hand
E S
ES
Plowman
J
J
Rampal
J B
JB
Safavy
A
A
Haugwitz
R D
RD
Narayanan
V L
VL
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D001386:Azides / Q000138:chemical synthesis* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D004355:Drug Stability; D005260:Female; D006207:Half-Life; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009374:Neoplasms, Experimental / Q000188:drug therapy; D011719:Pyrazines / Q000138:chemical synthesis* / Q000627:therapeutic use; D011739:Pyrimethamine / Q000031:analogs & derivatives*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology
D000970:Antineoplastic Agents; D001386:Azides; D011719:Pyrazines; D011743:Pyrimidines; C051397:pyrazine-2-diazohydroxide; C055910:3-azidopyrimethamine; D011739:Pyrimethamine