Synthesis and cytotoxic activity of N-(2-chloroethyl)-N-nitroureas and N-(2-chloroethyl)-N-nitrocarbamates.
As analogs of the widely used anti-tumor agents, N-(2-chloroethyl)-N-nitrosoureas, N-(2-chloroethyl)-N-nitroureas and N-(2-chloroethyl)-N-nitrocarbamates were synthesized by nitration following the reaction of the appropriate amines or alcohols with 2-chloroethyl isocyanate. All tested compounds exert cytotoxic effect with IC50 values of 10(-4) to 10(-6) M and most of them show somewhat higher cytotoxicity in nitrogen than in air.
Botyánszki
J
J
Research Group for Peptide Chemistry, Hungarian Academy of Sciences, Eötvös Lorand University, Budapest.
Bódi
J
J
Stratford
I J
IJ
Süli-Vargha
H
H
D000388:Air; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002219:Carbamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics*; D002330:Carmustine / Q000737:chemistry; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D006224:Cricetinae; D003412:Cricetulus; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D020128:Inhibitory Concentration 50; D009574:Nitro Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D009584:Nitrogen; D014508:Urea / Q000737:chemistry
D000970:Antineoplastic Agents; D002219:Carbamates; D009574:Nitro Compounds; D014508:Urea; D009584:Nitrogen; D002330:Carmustine