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• W2039821427 endingPage "3913" @default.
• W2039821427 startingPage "3900" @default.
• W2039821427 abstract "The cell surface aminopeptidase N (APN/CD13), overexpressed in tumor cells, plays a critical role in angiogenesis. However, potent, selective, and, particularly, noncytotoxic inhibitors ot this protein are lacking, and the present work was undertaken with the aim of developing a new generation of noncytotoxic inhibitors that bind to APN/CD13. In this context, we have synthesized a series of novel flavone-8-acetic acid derivatives. Among the herein described and evaluated compounds, the 2',3-dinitroflavone-8-acetic acid (19b) proved to be the most efficient and exhibited an IC(50) of 25 microM which is 2.5 times higher than that of bestatin (1), the natural known inhibitor of APN/CD13. However, in contrast to bestatin (1), the dinitroflavone 19b did not induce any cytotoxicity to cultured human model cells. The presence of other substituents such as NO(2) or OCH(3) groups at the 3'- or 4'-position of the B phenyl group, or the existence of steric constraints (compounds 24 and 29), did not improve selectivity and potency. The flavone 19b affinity for APN/CD13 is not recovered with other proteases such as matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE/CD143), neutral endopeptidase (NEP/CD10), gamma-glutamyl transpeptidase (CD224), or the serine proteases dipeptidyl peptidase IV (DPPIV/CD26) or cathepsin G." @default.
• W2039821427 created "2016-06-24" @default.
• W2039821427 creator A5029847938 @default.
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• W2039821427 creator A5081904211 @default.
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• W2039821427 date "2003-08-01" @default.
• W2039821427 modified "2023-10-03" @default.
• W2039821427 title "Synthesis and Biological Evaluation of Novel Flavone-8-acetic Acid Derivatives as Reversible Inhibitors of Aminopeptidase N/CD13" @default.
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• W2039821427 doi "https://doi.org/10.1021/jm021109f" @default.
• W2039821427 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/12930151" @default.
• W2039821427 hasPublicationYear "2003" @default.
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