| Title : Nitrobenzylcarbamate prodrugs of cytotoxic acridines for potential use with nitroreductase gene-directed enzyme prodrug therapy - Asche_2006_Bioorg.Med.Chem.Lett_16_1990 |
| Author(s) : Asche C , Dumy P , Carrez D , Croisy A , Demeunynck M |
| Ref : Bioorganic & Medicinal Chemistry Lett , 16 :1990 , 2006 |
|
Abstract :
The synthesis, solvolytic behaviour and cytotoxicity of novel 4-nitrobenzyl carbamates and carbonates derived from 3-amino-4-hydroxymethylacridine 1 are described. Compounds 2 and 6 are both substrates for Escherichia coli nitroreductase and the highly active lead structure 1 is liberated upon incubation of the two compounds in the presence of NTR and its cofactor NADH. Additionally, the cytostatic activity of 2 and 6 against human HT29 colon carcinoma cell lines is decreased 80-fold and 360-fold, respectively, indicating their suitability and potency as prodrugs for either gene-directed enzyme prodrug therapy or antibody-directed enzyme prodrug therapy. |
| PubMedSearch : Asche_2006_Bioorg.Med.Chem.Lett_16_1990 |
| PubMedID: 16442795 |
Asche C, Dumy P, Carrez D, Croisy A, Demeunynck M (2006)
Nitrobenzylcarbamate prodrugs of cytotoxic acridines for potential use with nitroreductase gene-directed enzyme prodrug therapy
Bioorganic & Medicinal Chemistry Lett
16 :1990
Asche C, Dumy P, Carrez D, Croisy A, Demeunynck M (2006)
Bioorganic & Medicinal Chemistry Lett
16 :1990