Nitroacridines with selective toxicity towards hypoxic mammalian cells: Synthesis and stability of tritiated derivatives
✍ Scribed by William A. Denny; David Chambers; Georgina M. Stewart; William R. Wilson
- Publisher
- John Wiley and Sons
- Year
- 1985
- Tongue
- French
- Weight
- 428 KB
- Volume
- 22
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
The clinically-used antitumour druq nitracrine ( 9-f3-d imethylaminopropvl] amino-1 -ni troacr idine ) shows increased toxicity towards mammalian tumour cells under hvpoxic conditions, .7ut several. closely-related nitroacridines do not show this selectivity. To aid studies of the mode of action of this class of compound four different tritium-labelled nitroacridines fG-3H] 9-amino-1-ni troacr idine , [G-3-9-methylamino-l-nitroacri~3ine, 9-( 3-(dimethylamino 1 propvlamino fG-3X] -1-ni troacridine I and 9-( 3-(dimethylamino 1 propylamino fG-3H) -3-ni troacri Aine were prepared from tritiated sodium N-( 3 ' -ni trophenyl ) anthrani late .
for addition of the amine sidechain to the intermediate chlotonitroacridines varied markedly for each derivative. The tritiated compounds proved stable as soli? salts, but dilute solutions rapidly hvdrolvsed to the nitroacridones, in a reaction which was assisted by liqht.