Combretastatin A-1
Combretastatin A-1 is a combretastatin and a stilbenoid. It can be found in Combretum caffrum, the Eastern Cape South African Bushwillow tree.[1]
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| IUPAC name
3-Methoxy-6-[(E)-2-(3,4,5-trimethoxyphenyl)ethenyl]benzene-1,2-diol | |
| Other names
Combretastatin A1; OXi4500 | |
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| Properties | |
| C18H20O6 | |
| Molar mass | 332.352 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
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Biological effects in mammals
It is an antiangiogenic agent acting by destabilizing tubulin, which induces cell apoptosis of proliferating endothelial cells.[1]
Derivatives as drugs
Currently designated an orphan drug by the FDA, combretastatin A1 diphosphate (OXi4503 or CA1P) is in Phase I clinical trials for relapsed and refractory acute myeloid leukemia and myelodysplastic syndrome.[2]
References
- Pettit, G. R.; Singh, S. B.; Niven, M. L.; Hamel, E.; Schmidt, J. M. (1987). "Isolation, Structure, and Synthesis of Combretastatins A-1 and B-1, Potent New Inhibitors of Microtubule Assembly, Derived from Combretum caffrum". Journal of Natural Products. 50 (1): 119–131. doi:10.1021/np50049a016. PMID 3598594.
- http://clinicaltrials.gov/ct2/show/NCT01085656
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