艾贝司他
外观
艾贝司他 | |
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IUPAC名 3-[(Dimethylamino)methyl]-N2-[4-(hydroxycarbamoyl)phenoxy]ethyl1-benzofuran-2-carboxamide | |
别名 | PCI-24781; CRA-024781 |
识别 | |
CAS号 | 783355-60-2 ![]() 783356-67-2((HCl)) ![]() |
PubChem | 11749858 |
ChemSpider | 9924562 |
SMILES |
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InChI |
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InChIKey | MAUCONCHVWBMHK-UHFFFAOYAM |
KEGG | D10060 |
性质 | |
化学式 | C21H23N3O5 |
摩尔质量 | 397.42 g·mol−1 |
若非注明,所有数据均出自标准状态(25 ℃,100 kPa)下。 |
艾贝司他(INN[1]:Abexinostat,前身为PCI-24781),也译为阿贝司他,是一种用于癌症治疗的实验性候选药物。[2]它由法莫斯利医药(Pharmacyclics)开发并授权给徐诺药业,并且正在进行B细胞淋巴瘤的II期临床试验。[3]临床前研究表明它还具有治疗不同类型癌症的潜力。[4][5][6][7]
艾贝司他作为一种泛组蛋白脱乙酰酶抑制剂发挥其作用[8][9]并抑制RAD51,后者参与修复DNA双链断裂。[10]
参考资料
[编辑]- ^ WHO Drug Information (页面存档备份,存于互联网档案馆), Vol. 25, No. 2, 2011
- ^ Abexinostat (页面存档备份,存于互联网档案馆), NCI Cancer Dictionary
- ^ Abexinostat HCl (PCI-24781), PanHDAC-inhibitor 互联网档案馆的存檔,存档日期2013-10-27., Pharmacyclics
- ^ Bhalla, S; Balasubramanian, S; David, K; Sirisawad, M; Buggy, J; Mauro, L; Prachand, S; Miller, R; Gordon, LI; Evens, AM. 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. 2009, 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. Combining PCI-24781, a novel histone deacetylase inhibitor, with chemotherapy for the treatment of soft tissue sarcoma. Clinical Cancer Research. 2009, 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. 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, 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. Histone deacetylase inhibitor (HDACI) PCI-24781 potentiates cytotoxic effects of doxorubicin in bone sarcoma cells. Cancer Chemotherapy and Pharmacology. 2011, 67 (2): 439–46. PMID 20461381. S2CID 1344662. 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. CRA-024781: A novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo. Molecular Cancer Therapeutics. 2006, 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. HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination. Proceedings of the National Academy of Sciences of the United States of America. 2007, 104 (49): 19482–7. Bibcode:2007PNAS..10419482A. PMC 2148315
. PMID 18042714. doi:10.1073/pnas.0707828104
.
- ^ NCI Drug Dictionary. National Cancer Institute. [2023-02-02]. (原始内容存档于2023-02-02) (英语).