CAS: 929016-96-6; (E)-3-(2-Butyl-1-(2-(Diethylamino)Ethyl)-1H-Benzo[d]Imidazol-5-yl)-N-Hydroxyacrylamide

该化合物是一种基于氢氧酸的直肠脱乙酰酶抑制剂,主要针对其在肿瘤治疗中的潜力进行调查,有选择地针对一,二和四类HDAC酶,调节基因表达方式,在恶性细胞中诱发人口中毒,临床和临床研究显示它在混合疗法中的效力,特别是急性近血性白血病(AML)和近距离性塑胶综合症(MDS)等血解恶性恶性肿瘤方面的功效.Pracinostat 展示了有利的药用植物动力特性,包括口服生物利用率和持续的目标接触.其行动机制加强了骨骼和非岩质蛋白的发炎,从而助长了其抗肿瘤效应.目前进行的研究继续探索其在固体肿瘤和其他血解障碍方面的治疗潜力.

结构式图片

上下游产品

3-[2-Butyl-1-(2-Diethylaminoethyl)-1H-Benzoimidazol-5-Yl]Acrylic Acid Methyl Ester 1056198-30-1

合成工艺路线路线简述

    📜Methyl (E)-3-(4-((2(Diethylamino)Ethyl)Amino)-3-Nitrophenyl)Acrylate置于n-甲基吗啉,三乙基硅烷,Tin(II) Chloride Dihdyrate,1-羟基苯并三唑,溶剂黄146,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三氟乙酸,Sodium Hydroxide体系中,用 四氢呋喃,甲醇,乙醇,二氯甲烷,水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 16.0H,反应生成 (2E)-3-[2-丁基-1-[2-(二乙基氨基)乙基]-1H-苯并咪唑-5-基]-N-羟基丙烯酰胺
    参考文献:控制异羟肟酸的血浆稳定性:Medchem工具箱
    标题:控制异羟肟酸的血浆稳定性:Medchem工具箱
    摘要:异羟肟酸是杰出的锌螯合基团,可用于设计各种治疗领域中的有效和选择性金属酶抑制剂.一些异羟肟酸显示出较高的血浆清除率,导致体内活性差,尽管它们在体外可能是非常有效的化合物.我们设计了一个由57名成员组成的异羟肟酸文库,以探索这些系列中结构与血浆的稳定性关系,并确定哪些酶和哪些药效团对血浆稳定性至关重要.芳基酯酶和羧酸酯酶被确定为异羟肟酸的主要代谢酶.最后,我们建议引入或删除结构特征以提高稳定性.因此,这项工作提供了第一个药物化学工具箱(实验程序和结构指导),用于评估和控制异羟肟酸的血浆稳定性,并充分发挥其作为体内药理探针和治疗剂的潜力.这项研究与临床前开发特别相关,因为它允许获得在人和啮齿动物模型中同样稳定的化合物.
    DOI:10.1021/acs.Jmedchem.7B01444

    海关参考信息

    专利信息


    专利号:US-2025235415-A1
    优先权日:2022-02-23
    标 题:Modulation of human breast milk composition
    发明人:ROSS MICHAEL G; DESAI MINA
    权利人:LUNDQUIST INST FOR BIOMEDICAL INNOVATION AT HARBOR UCLA MEDICAL CENTER
    摘要:Compositions and methods for improving a child, such as an infant's health, are provided. The methods entail improving the quality of breast milk in a female human individual that provides breast milk, or expects to provide breast milk, to the child, by administering to the individual an agent that increases the individual's sensitivity to insulin, and/or an agent that reduces the substrate uptake, synthesis or secretion of long chain fatty acids, reduces the substrate uptake, synthesis or secretion of short chain fatty acids, increases the amino acid uptake, protein synthesis or protein secretion of proteins, or reduces the uptake or synthesis of lactose.

    专利号:US-11286271-B2
    优先权日:2018-07-31
    标 题 :Iridium (III) complexes containing N-heterocyclic carbene ligand, synthesis, and their use thereof in cancer treatment
    发明人:CHE CHI MING; LAM TSZ LUNG; TONG KA CHUNG
    权利人:UNIV HONG KONG
    摘要:Provided herein are Ir(III) complexes comprising N-heterocyclic carbene ligand, method of synthesis of the Ir(III) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Ir(III) complexes under both dark and light conditions. Also provided is a method of detecting the Ir(III) complex in a biological system. Also provided is a method of making the Ir(III) complex. The Ir(III) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

    专利号:US-2024066133-A1
    优先权日:2020-03-06
    标 题 :Therapeutic agents and conjugates thereof
    发明人:SONG YUNTAO; LI ANRONG; LI HUI; LI XIANFENG; YANG JUNBAO
    权利人:BEIJING XUANYI PHARMASCIENCES CO LTD
    摘要:The present disclosure provides a class of conjugates of general formula (X), a class of TLR9 agonist derivatives, such as formula (I), (XX), and (XXI), certain diastereomers of STING agonists, a class of STING agonist derivatives, such as formula (XXVIV), a class of heterocyclic compounds of general formula (II), a class of heterocyclic compounds of general formula (III), as defined herein. A 1 , A 2 , T, Z 1 , Z 2 , Z 3 , b 1 , and b 2 , in formula (X) are defined herein. The conjugate provides unique properties that are based upon the properties of the therapeutic agents that are part of the conjugate. Also provided are methods of synthesis and use of compounds.

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    主要参考文献


    1: Garcia-Manero G, Kazmierczak M, Wierzbowska A, Fong CY, Keng MK, Ballinari G, Scarci F, Adès L. Pracinostat combined with azacitidine in newly diagnosed adult acute myeloid leukemia (AML) patients unfit for standard induction chemotherapy: PRIMULA phase III study. Leuk Res. 2024 May;140:107480. doi: 10.1016/j.leukres.2024.107480. Epub 2024 Mar 12.
    163:105274. doi: 10.1016/j.phrs.2020.105274. Epub 2020 Nov 7. 3(4):508-518. doi: 10.1182/bloodadvances.2018027409.
    4: Bose P, Swaminathan M, Pemmaraju N, Ferrajoli A, Jabbour EJ, Daver NG, DiNardo CD, Alvarado Y, Yilmaz M, Huynh-Lu J, Qiao W, Wang X, Matamoros A, Zhou L, Pierce S, Schroeder KD, Kantarjian HM, Verstovsek S. A phase 2 study of pracinostat combined with ruxolitinib in patients with myelofibrosis. Leuk Lymphoma. 2019 Jul;60(7):1767-1774. doi: 10.1080/10428194.2018.1543876. Epub 2019 Jan 11.

    合成参考文献


    参考文献:10.1007/s11864-017-0445-5
    摘要:Thomas X, Le Jeune C. Treatment of Elderly Patients With Acute Myeloid Leukemia. Current Treatment Options in Oncology. 2017 Jan 31;18(1):2. doi: 10.1007/s11864-017-0445-5.
    参考文献:10.1186/s12943-017-0596-9
    摘要:Toh TB, Lim JJ, Chow EK. Epigenetics in cancer stem cells. Molecular Cancer. 2017 Feb 01;16(1):29. doi: 10.1186/s12943-017-0596-9.
    参考文献:10.1016/j.ejmech.2020.112679
    摘要:Liu W, Liang Y, Si X. Hydroxamic acid hybrids as the potential anticancer agents: An Overview. European Journal of Medicinal Chemistry. 2020 Nov;205():112679. doi: 10.1016/j.ejmech.2020.112679.
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