Disease relevance of Nor-HN2

• A complex of Co(III) with a nitro group and a bis(2-chloroethyl)amine moiety was prepared in an effort to develop a new anticancer agent with radiosensitizing capabilities, direct antitumor activity, and the ability to interact positively with clinically relevant hyperthermia temperatures [1].
• Four urinary metabolites of the cytostatic drug cyclophosphamide were tested for mutagenicity in the Ames Salmonella assay: nornitrogen mustard (NM), 4-ketocyclophosphamide, 3-(2-chloroethyl)oxazolidone (OZ), and N,N'-bis(2-chloroethyl)piperazine [2].
• Estramustine-phosphate (EMP), a combination of nornitrogen mustard and 17 beta-estradiol, has been demonstrated to exert specific antiproliferative effects on human glioma cells in vitro [3].
• Upon exposure to E. coli beta-glucuronidase, fast hydrolysis occurs but a lower cytotoxicity against LoVo cancer cells is observed compared to the nornitrogen mustard alone [4].

High impact information on Nor-HN2

• Strong experimental and theoretical evidence was obtained to support the hypothesis that the P-N bond scission observed at neutral pH does not occur in the parent PM to produce nornitrogen mustard; rather it is an aziridinium ion derived from PM which undergoes P-N bond hydrolysis to give chloroethylaziridine [5].
• Nor-nitrogen mustard was more effective in inducing point mutation damage than nitrogen mustard and a reversal of potency was found for cytogenetic damage [6].
• In pH 7.4, 0.067 M sodium phosphate buffer at 37 degrees C, both phosphoramide mustard (PM) and nornitrogen mustard (NNM) were degraded in an apparent first-order fashion with half-lives of 24.8 and 14.5 min, respectively [7].
• A gas chromatographic (GC-ECD) method was developed for the determination of nornitrogen mustard (NOR) and its hydrolysis products [8].
• A theoretical study of H3PO4, nor-N-mustard, and cyclophosphamide [9].

References