Accessibility navigation


New prodrugs derived from 6-aminodopamine and 4-aminophenol as candidates for melanocyte-directed enzyme prodrug therapy (MDEPT)

Knaggs, S., Malkin, H., Osborn, H.M.I., Williams, N.A.O. and Yaqoob, P. (2005) New prodrugs derived from 6-aminodopamine and 4-aminophenol as candidates for melanocyte-directed enzyme prodrug therapy (MDEPT). Organic & Biomolecular Chemistry, 3 (21). pp. 4002-4010. ISSN 1477-0520

Full text not archived in this repository.

To link to this article DOI: 10.1039/b506404j

Abstract/Summary

Two novel tyrosinase mediated drug delivery pathways have been investigated for the selective delivery of cytotoxic units to melanocytes from urea and thiourea prodrugs. The synthesis of these prodrugs is reported, as well as oximetry data that illustrate that the targets are substrates for tyrosinase. The stability of each of the prodrugs in (i) phosphate buffer and (ii) bovine serum is discussed, and the urea prodrugs are identified as lead candidates for further studies. Finally, HPLC studies and preliminary cytotoxicity studies in a melanotic and an amelanotic cell line, that illustrate the feasibility of the approach, are presented.

Item Type:Article
Refereed:Yes
Divisions:Faculty of Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy
Faculty of Life Sciences > School of Chemistry, Food and Pharmacy > Department of Food and Nutritional Sciences
Interdisciplinary centres and themes > Institute for Cardiovascular and Metabolic Research (ICMR)
ID Code:13708
Uncontrolled Keywords:MALIGNANT-MELANOMA, ANTIMELANOMA ACTIVITY, TARGETED TREATMENT, TYROSINASE, N-ACETYL-4-S-CYSTEAMINYLPHENOL, MELANOGENESIS, ANALOGS, CELLS, CYTOTOXICITY, NITROGEN

Centaur Editors: Update this record

Page navigation