Synthesis and analysis of urea and carbamate prodrugs as candidates for melanocyte-directed enzyme prodrug therapy (MDEPT)

Allan M Jordan; Tariq H Khan; Hugh Malkin; Helen M I Osborn

Synthesis and analysis of urea and carbamate prodrugs as candidates for melanocyte-directed enzyme prodrug therapy (MDEPT)

Allan M Jordan, Tariq H Khan, Hugh Malkin, Helen M I Osborn

Cancer Research UK Manchester Institute

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

Abstract

The suitability of 4-di(2-chloroethyl)aminoanilino-4-hydroxyphenethylaminomethanone 2 to act as a prodrug for melanocyte-directed enzyme prodrug therapy (MDEPT) is assessed. Thus its synthesis, ability to generate a cytotoxic agent upon exposure to tyrosinase, and stability within different sera are reported. A comparison is made to illustrate that the new urea prodrug 2 is a more suitable candidate for MDEPT than the corresponding carbamate prodrug 1.

Original language	English
Pages (from-to)	2625-33
Number of pages	9
Journal	Bioorganic and Medicinal Chemistry
Volume	10
Issue number	8
Publication status	Published - Aug 2002

Keywords

Animals
Blood
Carbamates
Cattle
Cell Death
Drug Delivery Systems
Drug Stability
Enzymes
Humans
Melanocytes
Monophenol Monooxygenase
Prodrugs
Urea

Cite this

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title = "Synthesis and analysis of urea and carbamate prodrugs as candidates for melanocyte-directed enzyme prodrug therapy (MDEPT)",

abstract = "The suitability of 4-di(2-chloroethyl)aminoanilino-4-hydroxyphenethylaminomethanone 2 to act as a prodrug for melanocyte-directed enzyme prodrug therapy (MDEPT) is assessed. Thus its synthesis, ability to generate a cytotoxic agent upon exposure to tyrosinase, and stability within different sera are reported. A comparison is made to illustrate that the new urea prodrug 2 is a more suitable candidate for MDEPT than the corresponding carbamate prodrug 1.",

keywords = "Animals, Blood, Carbamates, Cattle, Cell Death, Drug Delivery Systems, Drug Stability, Enzymes, Humans, Melanocytes, Monophenol Monooxygenase, Prodrugs, Urea",

author = "Jordan, {Allan M} and Khan, {Tariq H} and Hugh Malkin and Osborn, {Helen M I}",

year = "2002",

month = aug,

language = "English",

volume = "10",

pages = "2625--33",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

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TY - JOUR

T1 - Synthesis and analysis of urea and carbamate prodrugs as candidates for melanocyte-directed enzyme prodrug therapy (MDEPT)

AU - Jordan, Allan M

AU - Khan, Tariq H

AU - Malkin, Hugh

AU - Osborn, Helen M I

PY - 2002/8

Y1 - 2002/8

N2 - The suitability of 4-di(2-chloroethyl)aminoanilino-4-hydroxyphenethylaminomethanone 2 to act as a prodrug for melanocyte-directed enzyme prodrug therapy (MDEPT) is assessed. Thus its synthesis, ability to generate a cytotoxic agent upon exposure to tyrosinase, and stability within different sera are reported. A comparison is made to illustrate that the new urea prodrug 2 is a more suitable candidate for MDEPT than the corresponding carbamate prodrug 1.

AB - The suitability of 4-di(2-chloroethyl)aminoanilino-4-hydroxyphenethylaminomethanone 2 to act as a prodrug for melanocyte-directed enzyme prodrug therapy (MDEPT) is assessed. Thus its synthesis, ability to generate a cytotoxic agent upon exposure to tyrosinase, and stability within different sera are reported. A comparison is made to illustrate that the new urea prodrug 2 is a more suitable candidate for MDEPT than the corresponding carbamate prodrug 1.

KW - Animals

KW - Blood

KW - Carbamates

KW - Cattle

KW - Cell Death

KW - Drug Delivery Systems

KW - Drug Stability

KW - Enzymes

KW - Humans

KW - Melanocytes

KW - Monophenol Monooxygenase

KW - Prodrugs

KW - Urea

M3 - Article

C2 - 12057651

SN - 0968-0896

VL - 10

SP - 2625

EP - 2633

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 8

ER -

Synthesis and analysis of urea and carbamate prodrugs as candidates for melanocyte-directed enzyme prodrug therapy (MDEPT)

Abstract

Keywords

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