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3,4-Dihydro-1H-[1,3]oxazino[4,5-c]acridines as a new family of cytotoxic drugs.

Authors :
Ouberai M
Asche C
Carrez D
Croisy A
Dumy P
Demeunynck M
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Sep 01; Vol. 16 (17), pp. 4641-3. Date of Electronic Publication: 2006 Jun 13.
Publication Year :
2006

Abstract

A series of [1,3]oxazino fused acridines has been prepared as precursors of cytotoxic 3-amino-4-hydroxymethylacridine 2. Their cytotoxic activity has been evaluated against HT29 colon carcinoma cell line and was shown to be dependent on the nature of the substituent located on position 2 of the oxazine ring. Additionally, the nitrophenyl derivative 3f is activated by nitroreductase, indicating its potency as prodrug for either gene-directed or antibody-directed enzyme prodrug therapies.

Details

Language :
English
ISSN :
0960-894X
Volume :
16
Issue :
17
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
16777412
Full Text :
https://doi.org/10.1016/j.bmcl.2006.05.101