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. Author manuscript; available in PMC: 2013 Feb 6.
Published in final edited form as: Molecules. 2012 Mar 26;17(4):3672–3689. doi: 10.3390/molecules17043672

Table 2.

Prodrug stability in capan-2 cell homogenate with the presence and the absence of inhibitors.

Prodrug Half Life (min)
Phosphate Buffer pH 7.4 Capan-2 Cell Homogenate Cathepsin D Inhibitor Aminopeptidase Inhibitor TPP 2 Inhibitor DPP 3 Inhibitor
5′-O-L-leucyl-L-glycylfloxuridine 23.1 ± 4.1§ 3.9 ± 1.1 7.9 ± 0.7 14.0 ± 4.3 5.6 ± 0.6 32.2 ± 9.3
5′-O-L-glycyl-L-leucylfloxuridine 35.7 ± 0.9§ 29.2 ± 0.7 32.2 ± 0.1 33.0 ± 0.4 21.0 ± 0.9 26.5 ± 17.5
5′-O-L-valyl-L-phenylalanyl- floxuridine 104.7 ± 7.0§ 56.2 ±12.8 76.4 ±6.1 93.6 ± 29.3 46.1 ± 1.9 67.7 ± 15.1
5′-O-L-phenylalanyl-L-tyrosyl- floxuridine 233.9 ± 6.6§ 42.8 ± 0.0 105.7 ± 12.8* 54.7 ± 2.8 42.2 ± 1.3 47.2 ± 3.6
5′-O-L-phenylalanyl-L-glycyl- floxuridine 132.1 ± 10.2§ 4.3 ± 0.9 10.2 ± 3.0 25.7 ± 0.4* 19.6 ± 0.4* 30.1 ± 10.0
5′-O-L-phenylalanylfloxuridine 187.0 ± 19.0§ 3.0 ± 0.1 60.6 ± 4.6* 48.7 ± 0.37* 15.3 ± 0.6* 28.9 ± 10.7
*

<0.01; cathepsin D inhibitor–pepstatin A, aminopeptidase inhibitor–puromycin, TPP2 (tripeptidylpepptidase 2) inhibitor-H-Ala-Ala-Phe-CMK CF3CO2H, DPP3 (dipeptidylpeptidase 3)–1,10-phenanthroline. Asterisks indicate significant difference in half lives in capan-2 cell homogenate with an inhibitor to ones without inhibitors. Values presented are the mean ± s.d. (* p < 0.01; t-test).

§

from Reference [50].