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3,4-Dihydro-1H-[1,3]oxazino[4,5-c]acridines as a new family of cytotoxic drugs.
- 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.
- Subjects :
- Acridines chemical synthesis
Acridines classification
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Antineoplastic Agents toxicity
Cell Line, Tumor
Cell Survival drug effects
Humans
Molecular Structure
Structure-Activity Relationship
Acridines chemistry
Acridines toxicity
Hydrogen chemistry
Oxazines chemistry
Subjects
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