維基百科

艾貝司他

化合物

艾貝司他（INN[1]：Abexinostat，前身為PCI-24781），也譯為阿貝司他，是一種用於癌症治療的實驗性候選藥物。[2]它由法莫斯利醫藥（Pharmacyclics）開發並授權給徐諾藥業，並且正在進行B細胞淋巴瘤的II期臨床試驗。[3]臨床前研究表明它還具有治療不同類型癌症的潛力。[4][5][6][7]

艾貝司他
IUPAC名
3-[(Dimethylamino)methyl]-N2-[4-(hydroxycarbamoyl)phenoxy]ethyl1-benzofuran-2-carboxamide
別名 PCI-24781; CRA-024781
識別
CAS號 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
性質
化學式 C21H23N3O5
摩爾質量 397.42 g·mol−1
若非註明，所有數據均出自標準狀態（25 ℃，100 kPa）下。

艾貝司他作為一種泛組蛋白脫乙酰酶抑制劑發揮其作用[8][9]並抑制RAD51，後者參與修復DNA雙鏈斷裂。[10]

參考資料

編輯
  1. ^ WHO Drug Information （頁面存檔備份，存於互聯網檔案館）, Vol. 25, No. 2, 2011
  2. ^ Abexinostat （頁面存檔備份，存於互聯網檔案館）, NCI Cancer Dictionary
  3. ^ Abexinostat HCl (PCI-24781), PanHDAC-inhibitor 互聯網檔案館的存檔，存檔日期2013-10-27., Pharmacyclics
  4. ^ 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. 
  5. ^ 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  . 
  6. ^ 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  . 
  7. ^ 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. 
  8. ^ 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  . 
  9. ^ 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  . 
  10. ^ NCI Drug Dictionary. National Cancer Institute. [2023-02-02]. （原始內容存檔於2023-02-02） （英語）. 

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