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Tariq Hussain Khan

Patrick Anthony Riley

Andrew Photiou

Hugh Malkin

Helen Mary Osborn

Helen Mary Isted Osborn

Novel mono- and dihydroxy phenylethylamine derivatives useful in treating melanoma are provided having the formulae (Ia, Ib or Ic). In the above formulae, Ris hydrogen or &#x2014;COOR, Ris hydrogen or Calkyl; Rand Rindependently represent hydrogen and hydroxy, Ris hydrogen, C1&#x2013;4? alkyl or halogen, X is &#x2014;CHOH&#x2014;, &#x2014;CH-oxygen or sulphur, m is zero or 1, W is oxygen or sulphur, and &#x2014;ODrug, &#x2014;NHDrug and &#x2014;N(Drug)each represent a residue of a therapeutically active agent. The above compounds are prodrugs which are inactive until metabolised by enzymes expressed by host melanoma cells. The invention allows a greater amount of active agent to be used while reducing systemic side effects 

Phenylethylamine derivatives and their use in the treatment of melanoma

Novel pro-drugs and assay reagents are provided which are useful as therapeutic agents especially for delivery and targetting therapeutically active agents to melanoma cells. The pro-drugs and assay reagents are substrates for tyrosinase and may be represented by the formula TyrX&mdash;B&mdash;ThrAg*. The compounds of formula TyrX&mdash;B&mdash;ThrAg* are capable of releasing a therapeutically active agent or assayable substance (ThrAg) at a desired location. TyrX&mdash; being a residue of an optionally substituted tyrosine analogue.

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Bishop Stortford, United Kingdom

Tariq Hussain Khan