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

AM Jordan, TH Khan, H Malkin, HMI Osborn

文献索引:Jordan, Allan M; Khan, Tariq H; Malkin, Hugh; Osborn, Helen M I Bioorganic and medicinal chemistry, 2002 , vol. 10, # 8 p. 2625 - 2633

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被引用次数: 48

摘要

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 ...