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

Sarah Knaggs; Hugh Malkin; Helen M I Osborn; Nana Aba O Williams; Parveen Yaqoob

doi:10.1039/b506404j

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

Sarah Knaggs, Hugh Malkin, Helen M I Osborn, Nana Aba O Williams, Parveen Yaqoob

Dentistry

Research output: Contribution to journal › Article › peer-review

28 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	4002-10
Number of pages	9
Journal	Organic and Biomolecular Chemistry
Volume	3
Issue number	21
DOIs	https://doi.org/10.1039/b506404j
Publication status	Published - 2005

Access to Document

10.1039/b506404j

Cite this

@article{f9623f4b918c489291d4ec2d1997e53c,

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

abstract = "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.",

author = "Sarah Knaggs and Hugh Malkin and Osborn, {Helen M I} and Williams, {Nana Aba O} and Parveen Yaqoob",

year = "2005",

doi = "10.1039/b506404j",

language = "English",

volume = "3",

pages = "4002--10",

journal = "Organic and Biomolecular Chemistry",

issn = "1477-0520",

publisher = "Royal Society of Chemistry",

number = "21",

}

TY - JOUR

T1 - New prodrugs derived from 6-aminodopamine and 4-aminophenol as candidates for melanocyte-directed enzyme prodrug therapy (MDEPT)

AU - Knaggs, Sarah

AU - Malkin, Hugh

AU - Osborn, Helen M I

AU - Williams, Nana Aba O

AU - Yaqoob, Parveen

PY - 2005

Y1 - 2005

N2 - 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.

AB - 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.

U2 - 10.1039/b506404j

DO - 10.1039/b506404j

M3 - Article

C2 - 16240021

SN - 1477-0520

VL - 3

SP - 4002

EP - 4010

JO - Organic and Biomolecular Chemistry

JF - Organic and Biomolecular Chemistry

IS - 21

ER -

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

Abstract

Access to Document

Fingerprint

Cite this