Enzyme activated anti-tumor agents conjugates of p-Hydroxyaniline mustard (cas 1204-69-9) as substrates for hydrolytic enzymes
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Add time:07/18/2019 Source:sciencedirect.com
The O-phosphate, O-sulphate and O-glucuronide of p-hydroxyaniline mustard were synthesised with the objective that they might be selective anti-tumour agents for tumours with high levels of phosphatase, sulphatase and glucuronidase respectively. This paper shows that the O-phosphate and O-glucuronide can be deconjugated by the appropriate enzymes in vitro to release the rapidly reacting p-hydroxyaniline mustard. The O-sulphate however proved refractory to hydrolysis by all aryl sulphatases tested.
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