Perry, Maria de Jesus; Carvalho, Emília; Rosa, Eduarda and Iley, Jim
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|DOI (Digital Object Identifier) Link:||http://doi.org/10.1016/j.ejmech.2008.06.022|
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A series of 3-[a-(acylamino)acyl]-1-aryl-3-methyltriazenes 6ael, potential cytotoxic triazene prodrugs, were synthesised by coupling 1-aryl- 3-methyltriazenes to N-acylamino acids. Their hydrolysis was studied in isotonic pH 7.4 phosphate buffer and in human plasma, while hydrolysis of the derivative 6a was studied in more depth across a range of pH values. Prodrugs 6ael hydrolyse by cleavage of the triazene acyl group to afford the corresponding monomethyltriazenes. Studies in human plasma demonstrate that acylation of the a-amino group of the amino acid carrier is an effective means of reducing the chemical reactivity of the a-aminoacyl derivatives while retaining a rapid rate of enzymatic hydrolysis. These derivatives displayed log P values that suggest they should be well absorbed through biological membranes.
|Item Type:||Journal Article|
|Copyright Holders:||2008 Elsevier Masson SAS.|
|Academic Unit/Department:||Faculty of Science, Technology, Engineering and Mathematics (STEM) > Life, Health and Chemical Sciences
Faculty of Science, Technology, Engineering and Mathematics (STEM)
|Depositing User:||James Iley|
|Date Deposited:||24 Mar 2009 10:38|
|Last Modified:||05 Aug 2016 03:05|
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