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Abexinostat 
Summary
Abexinostat (INN,[2] anteriormente PCI-24781 o CRA-024781) con fórmula C21H23N3O5, es un candidato a fármaco experimental para el tratamiento del cáncer.[3] Actualmente se encuentra en desarrollo por Pharmacyclics y se encuentra en ensayos clínicos de fase II para el linfoma de células B.[4] Los estudios pre-clínicos sugieren también el potencial para el tratamiento de otros diferentes tipos de cáncer.[5][6][7][8]
| Abexinostat (Tosilato de Abexinostat) | ||
|---|---|---|
 | ||
| General | ||
| Fórmula estructural |
| |
| Fórmula molecular | ?H23N3O5 | |
| Identificadores | ||
| Número CAS | 783355-60-2[1] | |
| ChEBI | 92223 | |
| ChEMBL | CHEMBL2103863 | |
| ChemSpider | 9924562 | |
| DrugBank | DB12565 | |
| PubChem | 11749858 | |
| UNII | IYO470654U | |
| KEGG | D10060 | |
|
O=C(NO)c3ccc(OCCNC(=O)c2oc1ccccc1c2CN(C)C)cc3
| ||
|
InChI=1S/C21H23N3O5/c1-24(2)13-17-16-5-3-4-6-18(16)29-19(17)21(26)22-11-12-28-15-9-7-14(8-10-15)20(25)23-27/h3-10,27H,11-13H2,1-2H3,(H,22,26)(H,23,25)
Key: MAUCONCHVWBMHK-UHFFFAOYSA-N | ||
Abexinostat ejerce su efecto como un inhibidor de la Histona deacetilasa.[9][10]
Referencias
editar- ↑ Número CAS
- ↑ WHO Drug Information, Vol. 25, No. 2, 2011
- ↑ Abexinostat, NCI Cancer Dictionary
- ↑ Abexinostat HCl (PCI-24781), PanHDAC-inhibitor Archivado el 27 de octubre de 2013 en Wayback Machine., Pharmacyclics
- ↑ Bhalla, S; Balasubramanian, S; David, K; Sirisawad, M; Buggy, J; Mauro, L; Prachand, S; Miller, R; Gordon, LI; Evens, AM (2009). «PCI-24781 induces caspase and reactive oxygen species-dependent apoptosis through NF-kappaB mechanisms and is synergistic with bortezomib in lymphoma cells». Clinical cancer research : an official journal of the American Association for Cancer Research 15 (10): 3354-65. PMC 2704489. PMID 19417023. doi:10.1158/1078-0432.CCR-08-2365.
- ↑ Lopez, G; Liu, J; Ren, W; Wei, W; Wang, S; Lahat, G; Zhu, QS; Bornmann, WG; McConkey, DJ; Pollock, RE; Lev, DC (2009). «Combining PCI-24781, a novel histone deacetylase inhibitor, with chemotherapy for the treatment of soft tissue sarcoma». Clinical cancer research : an official journal of the American Association for Cancer Research 15 (10): 3472-83. PMID 19417021. doi:10.1158/1078-0432.CCR-08-2714.
- ↑ Rivera-Del Valle, N; Gao, S; Miller, CP; Fulbright, J; Gonzales, C; Sirisawad, M; Steggerda, S; Wheler, J; Balasubramanian, S; Chandra, J (2010). «PCI-24781, a Novel Hydroxamic Acid HDAC Inhibitor, Exerts Cytotoxicity and Histone Alterations via Caspase-8 and FADD in Leukemia Cells». International journal of cell biology 2010: 207420. PMC 2817379. PMID 20145726. doi:10.1155/2010/207420.
- ↑ Yang, C; Choy, E; Hornicek, FJ; Wood, KB; Schwab, JH; Liu, X; Mankin, H; Duan, Z (2011). «Histone deacetylase inhibitor (HDACI) PCI-24781 potentiates cytotoxic effects of doxorubicin in bone sarcoma cells». Cancer chemotherapy and pharmacology 67 (2): 439-46. PMID 20461381. doi:10.1007/s00280-010-1344-7.
- ↑ Buggy, JJ; Cao, ZA; Bass, KE; Verner, E; Balasubramanian, S; Liu, L; Schultz, BE; Young, PR; Dalrymple, SA (2006). «CRA-024781: A novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo». Molecular cancer therapeutics 5 (5): 1309-17. PMID 16731764. doi:10.1158/1535-7163.MCT-05-0442.
- ↑ Adimoolam, S; Sirisawad, M; Chen, J; Thiemann, P; Ford, JM; Buggy, JJ (2007). «HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination». Proceedings of the National Academy of Sciences of the United States of America 104 (49): 19482-7. PMC 2148315. PMID 18042714. doi:10.1073/pnas.0707828104.
Datos: Q4667249
