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艾贝司他

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艾贝司他
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  checkY
783356-67-2（(HCl)）  checkY
PubChem 11749858
ChemSpider 9924562
SMILES
 
  • O=C(NO)c3ccc(OCCNC(=O)c2oc1ccccc1c2CN(C)C)cc3
InChI
 
  • 1/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)
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]
  1. ^ WHO Drug Information （页面存档备份，存于互联网档案馆）, Vol. 25, No. 2, 2011
  2. ^ Abexinostat （页面存档备份，存于互联网档案馆）, NCI Cancer Dictionary
  3. ^ Abexinostat HCl (PCI-24781), PanHDAC-inhibitor: B-cell Lymphoma. Pharmacyclics. [2025-01-31] （英语）. 
  4. ^ Bhalla, Savita; Balasubramanian, Sriram; David, Kevin; Sirisawad, Mint; Buggy, Joseph; Mauro, Lauren; Prachand, Sheila; Miller, Richard; Gordon, Leo I.; Evens, Andrew M. PCI-24781 Induces Caspase and Reactive Oxygen Species–Dependent Apoptosis Through NF-κB Mechanisms and Is Synergistic with Bortezomib in Lymphoma Cells. Clinical Cancer Research. 2009-05-15, 15 (10): 3354-3365. ISSN 1078-0432. PMC 2704489 可免费查阅. PMID 19417023. doi:10.1158/1078-0432.CCR-08-2365 （英语）. 
  5. ^ Lopez, Gonzalo; Liu, Juehui; Ren, Wenhong; Wei, Wei; Wang, Suizhao; Lahat, Guy; Zhu, Quan-Sheng; Bornmann, William G.; McConkey, David J.; Pollock, Raphael E.; Lev, Dina C. Combining PCI-24781, a Novel Histone Deacetylase Inhibitor, with Chemotherapy for the Treatment of Soft Tissue Sarcoma. Clinical Cancer Research. 2009-05-15, 15 (10): 3472-3483. ISSN 1078-0432. PMID 19417021. doi:10.1158/1078-0432.CCR-08-2714 （英语）. 
  6. ^ Rivera-Del Valle, Nilsa; Gao, Shan; Miller, Claudia P.; Fulbright, Joy; Gonzales, Carolina; Sirisawad, Mint; Steggerda, Susanne; Wheler, Jennifer; Balasubramanian, Sriram; Chandra, Joya. 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 (1): 207-420. ISSN 1687-8884. PMC 2817379 可免费查阅. PMID 20145726. doi:10.1155/2010/207420 （英语）. 
  7. ^ Yang, Cao; Choy, Edwin; Hornicek, Francis J.; Wood, Kirkham B.; Schwab, Joseph H.; Liu, Xianzhe; Mankin, Henry; Duan, Zhenfeng. Histone deacetylase inhibitor (HDACI) PCI-24781 potentiates cytotoxic effects of doxorubicin in bone sarcoma cells. Cancer Chemotherapy and Pharmacology. 2011-02, 67 (2): 439-446. ISSN 0344-5704. PMID 20461381. S2CID 1344662. doi:10.1007/s00280-010-1344-7 （英语）. 
  8. ^ Buggy, Joseph J.; Cao, Z. Alexander; Bass, Kathryn E.; Verner, Erik; Balasubramanian, Sriram; Liu, Liang; Schultz, Brian E.; Young, Peter R.; Dalrymple, Stacie A. CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo. Molecular Cancer Therapeutics. 2006-05-01, 5 (5): 1309-1317. ISSN 1535-7163. PMID 16731764. doi:10.1158/1535-7163.MCT-05-0442 （英语）. 
  9. ^ Adimoolam, Shanthi; Sirisawad, Mint; Chen, Jun; Thiemann, Patti; Ford, James M.; Buggy, Joseph J. HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination. Proceedings of the National Academy of Sciences. 2007-12-04, 104 (49): 19482-19487. Bibcode:2007PNAS..10419482A. ISSN 0027-8424. PMC 2148315 可免费查阅. PMID 18042714. doi:10.1073/pnas.0707828104 （英语）. 
  10. ^ NCI Drug Dictionary. National Cancer Institute. [2023-02-02]. （原始内容存档于2023-02-02） （英语）. 

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