Amsacrine
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| File:Amsacrine.svg | |
| Systematic (IUPAC) name | |
|---|---|
|
N-(4-(acridin-9-ylamino)-3-methoxyphenyl)methanesulfonamide | |
| Pharmacokinetic data | |
| Protein binding | 96 to 98% |
| Biological half-life | 8-9 hours |
| Identifiers | |
| CAS Number | 51264-14-3 |
| ATC code | L01XX01 (WHO) |
| PubChem | CID 2179 |
| DrugBank | APRD00064 |
| ChemSpider | 2094 |
| Chemical data | |
| Formula | C21H19N3O3S |
| Molar mass | 393.46 g/mol[[Script error: No such module "String".]] |
| Script error: No such module "collapsible list". | |
| (verify) | |
Amsacrine is an antineoplastic agent.
It has been used in acute lymphoblastic leukemia.[1]
Mechanism
Its planar fused ring system can intercalate into the DNA of tumor cells, thereby altering the major and minor groove proportions. These alterations to DNA structure inhibit both DNA replication and transcription by reducing association between the affected DNA and: DNA polymerase, RNA polymerase and transcription factors.
Amsacrine also expresses topoisomerase inhibitor activity, specifically inhibiting topoisomerase II (compares with the better known agent etoposide).[2]
References
- ↑ PMID 16330449
- ↑ Genetic Response to Metals. Sarkar, Bibudhendra. CRC Press, 1995. ISBN 9780824796150
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