CAS: 1316215-12-9; 2-((2-Chlorophenyl)(Phenyl)Amino)-N-(7-(Hydroxyamino)-7-Oxoheptyl)Pyrimidine-5-Carboxamide

该化合物是一种化学化合物,可用作直肠脱乙酰酶抑制剂,众所周知,HDAC抑制剂在改变对基因表达和细胞过程有影响的直ones的胃状态方面起着作用;该化合物的特点是,它能够有选择地抑制某些HDAC酶,从而推动直ones和非岩蛋白的摄取;由此产生的基因表达变化可能对各种生物环境产生重大影响,包括癌症治疗,...

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    专利信息


    专利号:US-11666569-B2
    优先权日:2013-10-24
    标题 :Treatment of polycystic diseases with an HDAC6 inhibitor
    发明人：GRADILONE SERGIO A; LARUSSO NICHOLAS F
    权利人:MAYO FOUND MEDICAL EDUCATION & RES; NAT INSTITUTES OF HEALTH NIH U S DEPT OF HEALTH AND HUMAN SERVICES DHHS U S GOVERNMENT
    摘要:An HDAC6-specific inhibitor (i.e., a compound of Formula I or II) is shown to reduce the pathogenesis associated with polycystic disease. Administration of an HDAC6-specific inhibitor attenuated many of the symptoms characteristic of polycystic liver disease including cyst formation, cyst growth and cholangiocyte proliferation. Treatment with a HDAC6-specific inhibitor also increased the amount of bile duct acetylated tubulin and β-catenin phosphorylation and/or acetylation while reducing bile duct β-catenin synthesis. These results demonstrate that HDAC6 is overexpressed in cystic cholangiocytes and that its pharmacological inhibition reduces cholangiocyte proliferation and cyst growth.

    专利号:US-10144714-B2
    优先权日:2015-06-08
    标 题 :Methods of making protein deacetylase inhibitors
    发明人：SEYEDI FARZANEH; VAN DUZER JOHN H
    权利人:ACETYLON PHARMACEUTICALS INC
    摘要:The present invention relates to methods and intermediates useful for the synthesis of protein deacetylase inhibitors.

    专利号:US-2023310400-A9
    优先权日:2018-07-23
    标题 :Synthesis of small molecule histone deacetylase 6 degraders, compounds formed thereby, and pharmaceutical compositions containing them

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    主要参考文献


    1: Pulya S, Amin SA, Adhikari N, Biswas S, Jha T, Ghosh B. HDAC6 as privileged target in drug discovery: A perspective. Pharmacol Res. 2021 Jan;163:105274. doi: 10.1016/j.phrs.2020.105274. Epub 2020 Nov 7. 25(5-6):370-387. doi: 10.1007/s10495-020-01607-3.
    3: Gordon MS, Shapiro GI, Sarantopoulos J, Juric D, Lu B, Zarotiadou A, Connarn JN, Le Bruchec Y, Dumitru CD, Harvey RD. Phase Ib Study of the Histone Deacetylase 6 Inhibitor Citarinostat in Combination With Paclitaxel in Patients With Advanced Solid Tumors. Front Oncol. 2022 Jan 7;11:786120. doi: 10.3389/fonc.2021.786120.
    4: Wu CP, Hung CY, Lusvarghi S, Chang YF, Hsiao SH, Huang YH, Hung TH, Yu JS, Ambudkar SV. Overexpression of Human ABCB1 and ABCG2 Reduces the Susceptibility of Cancer Cells to the Histone Deacetylase 6-Specific Inhibitor Citarinostat. Int J Mol Sci. 2021 Mar 5;22(5):2592. doi: 10.3390/ijms22052592.

    合成参考文献


    参考文献:10.1007/978-981-33-6314-4_3
    摘要:Wani MY, Malik MA. Treatment Modalities. 2021. In: Gold and its Complexes in Anticancer Chemotherapy.
    参考文献:10.1007/978-981-15-8179-3_8
    摘要:Ganai SA. Conspectus of Structurally Distinct Groups of Histone Deacetylase Inhibitors of Classical Histone Deacetylases and Sirtuins. 2020. In: Histone Deacetylase Inhibitors in Combinatorial Anticancer Therapy.
    参考文献:10.1007/978-3-031-33871-7_2
    摘要:Khatun S, Amin SA, Gayen S, Jha T. In Silico Discovery of Class IIb HDAC Inhibitors: The State of Art. 2023. In: Challenges and Advances in Computational Chemistry and Physics.
    参考文献:10.1007/978-981-19-9925-3_4
    摘要:Roy M, Biswas J, Datta A. Breast Cancer Therapy and Control. 2023. In: Genetics and Epigenetics of Breast Cancer.
    参考文献:10.1007/s42764-025-00154-y
    摘要:Jiang W, Liu S, Fu L. HDAC6 as a therapeutic target for HPV E7-driven cervical cancer. GENOME INSTAB. DIS. 2025 Mar 26;6(2):117–28. doi: 10.1007/s42764-025-00154-y.
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