Utilize este identificador para referenciar este registo: http://hdl.handle.net/10451/20945
Título: Dopamine- and tyramine-based derivatives of triazenes
Activation by tyrosinase and implications for prodrug design
Autor: Perry, M. Jesus
Mendes, Eduarda
Simplicio, Ana Luisa
Coelho, Ana
Soares, Ricardo V.
Iley, Jim
Moreira, Rui
Francisco, Ana Paula
Palavras-chave: Chemistry, Medicinal
Data: 2009
Editora: ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citação: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - Vol. 44, n. 8 (AUG 2009), p. 3228-3234
Resumo: A range of triazene derivatives were synthesized and investigated as prodrug candidates for melanocyte-directed enzyme prodrug therapy (MDEPT). The prodrugs contained a tyramine or dopamine promoiety required for tyrosinase activation and this was joined via a urea functional group to the cytotoxic triazene. The stability of each of the prodrugs in phosphate buffer, human plasma and in mushroom tyrosinase is discussed. The identification of the main peak formed after the tyrosinase reaction was attempted by LC-MS and the conversion of prodrug to the quinone was confirmed. (C) 2009 Elsevier Masson SAS. All rights reserved.. - Fundacao para a Ciencia e Tecnologia (Portugal). - The authors thank the Fundacao para a Ciencia e Tecnologia (Portugal) for financial support through their pluriannual funding to the iMed.UL research unit.
URI: http://hdl.handle.net/10451/20945
DOI: http://dx.doi.org/10.1016/j.ejmech.2009.03.025
ISSN: 0223-5234
Aparece nas colecções:FF - Produção Científica 2000-2009

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