Exisulind
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Names | |
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IUPAC name
2-[(1Z)-5-fluoro-1-[(4-methanesulfonylphenyl)methylidene]-2-methyl-1H-inden-3-yl]acetic acid
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Other names
Sulindac sulfone, Aptosyn, FGN-1, Prevatac
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Identifiers | |
59973-80-7 | |
ChEBI | CHEBI:64212 |
ChEMBL | ChEMBL488025 |
ChemSpider | 4582441 |
Jmol 3D model | Interactive image |
PubChem | 5472495 |
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Properties | |
Molar mass | 372.41 g/mol |
Vapor pressure | {{{value}}} |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Infobox references | |
Exisulind (tentative trade name Aptosyn) is an antineoplastic agent. It acts by inhibiting the enzyme cyclic guanosine monophosphate phosphodiesterase type 5 (EC 3.1.4.17).[1] It is the sulfone derivative of sulindac, an NSAID. Unlike sulindac, it has known effects on prostaglandin synthesis.[2] It was developed as the potential treatment of several conditions including familial adenomatous polyposis (FAP), precancerous sporadic colonic polyps, cervical dysplasia and the prevention of tumor recurrence in prostate and breast cancer.[3] Exisulind inhibits the enzyme cGMP-PDE, overexpressed in precancerous and cancerous colorectal cells, and induces apoptosis in such cells with minimal effects on normal cells. This apoptotic effect is independent of COX-1 or COX-2 inhibition, p53, Bcl-2, or cell cycle arrest. Preclinical evidence suggests that exisulind also inhibits angiogenesis.[4]
See also
References
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- Antineoplastic drugs
- Sulfones
- Carboxylic acids
- Indenes
- Antineoplastic and immunomodulating drug stubs