CAS: 29745-04-8; Rel-(3Ar,4R,7S,7As)-Hexahydro-4,7-Epoxyisobenzofuran-1,3-Dione

该化合物是来自甘巴里(Capharidin)的化学化合物,它是从泡泡虫中获取的天然产品,被归类为类,以其潜在的药用特性而著称,特别是在癌症研究中.诺康沙丁表现出了在室温温度下无色的黄色固体,水溶性相对较低,但有机溶剂的溶性较高.该化合物因其能抑制肿瘤生长并诱发癌症细胞的吸附性,因此成为药物学研究的一个主题.其行动机制涉及细胞过程的中断,特别是细胞分裂和存活.此外,诺卡萨丁因其潜在的抗炎和抗病毒特性而有所发现.然而,由于该化合物的毒性和潜在副作用,必须小心处理该化合物.研究仍在继续,诺卡里丁可能提供各种疾病新治疗方法的见解.

结构式图片

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合成工艺路线路线简述

    📜Exo-3,6-Epoxy-1,2,3,6-Tetrahydrophthalic Anhydride 在 Palladium 10% On Activated Carbon,氢气体系中,用 丙酮作为反应溶剂,50.0 °C,5.0 Mpa 条件下,以100%的收率获得norcantharidin
    参考文献:A Flow Chemistry Approach To Norcantharidin Analogues
    标题:A Flow Chemistry Approach To Norcantharidin Analogues
    摘要:利用 Thalesnano H-Cube™ 流动氢化器,采用 "一步法 "合成程序制备了酸酯和酸酰胺去甲蒽啶衍生物.传统上,这些类似物的快速库生成和反应放大受到 5,6-Dehydronorcantharidin批量氢化的限制.使用流动化学方法解决了这一问题.由于不存在相关的放大问题,我们设计出了一种方法,可以在生物筛选所需的任何规模上生产去甲蒽啶以及酸酯和酸酰胺类似物.
    Doi:10.2174/157018011795906730

    海关参考信息

    专利信息


    专利号:US-8835658-B2
    优先权日:2012-12-28
    标 题:Asymmetric synthesis of norcantharidin analougus by alkynylation of oxabenzonorbornadienes and their anticancer activities
    发明人:CHAN ALBERT SUN-CHI; FAN BAOMIN; WANG JUN; LIN CHENGYUAN; HUANG CHAO; YANG QINGJING; XU JIANBIN; BIAN ZHAOXIANG; LU AIPING; HU JUN
    权利人:UNIV HONG KONG BAPTIST; UNIV YUNNAN NATIONALITIES
    摘要:The present invention relates to a type of norcantharidin analogues and a method to synthesis such norcantharidin analogues by transition metal-catalyzed alkynylation of 7-oxabenzonorbornadienes. The present invention also relates to the use of such norcantharidin analogues in manufacture of a medicament for the treatment of cancer tumors.

    专利号:US-6110907-A
    优先权日:1997-04-30
    标题 :Synthesis of platinum complexes and uses thereof
    发明人:AU-YEUNG STEVE C F; HO YEE PING; GE LIN; XIUWEN HAN; XINNING WANG; SHIWEI LU; TAO JIANG
    权利人:DALIAN CHEMICAL PHYSICS INST; UNIV HONG KONG CHINESE
    摘要:This invention provides novel antitumor demethylcantharidin platinum complexes. This invention also provides a composition comprising at least one of said demethylcantharidin platinum complexes and a suitable carrier. This invention provides a pharmaceutical composition comprising effective amount of at least one of the said demethylcantharidin platinum complexes and a pharmaceutically acceptable carrier. This invention provides a method of inhibiting the growth of tumorous cells comprising contacting the cells with an amount of said demethylcantharidin platinum complex effective to inhibit the growth of said tumorous cells. This invention provides a method of inhibiting the growth of tumorous cells in a subject comprising administering to the subject with an amount of the said demethylcantharidin platinum complexes effective to inhibit the growth of said tumorous cells in the subject. Finally, this invention provides methods for producing said demethylcantharidin platinum complexes.

    专利号:US-12201669-B2
    优先权日:2021-03-11
    标 题:Small molecule suppressors of APOE gene expression and cerebral vascular amyloid pathology
    发明人:TSAI LI-HUEI; BLANCHARD JOEL
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:The present disclosure provides methods of inhibiting amyloid synthesis in a subject using small molecule inhibitors. The invention also includes methods of treating disease associated with amyloid synthesis, such as Alzheimer's disease. The small molecule inhibitors disclosed herein are compounds which are non-immunosuppressant cyclosporin including the pharmaceutically acceptable salts thereof.

    专利号:CN-115353522-A
    优先权日:2022-08-22
    标 题:Regioselective Synthesis of Icaritin-Norcantharidin Conjugate and Its Antitumor Application

    专利号:WO-9849174-A1
    优先权日:1997-04-30
    标 题:Synthesis of platinum complexes and uses thereof

    专利号:CN-111303179-A
    优先权日:2020-03-17
    标 题:Synthesis of a Class of Norcantharidin Carboxylic Acid Difluorobenzyl Esters and Its Antitumor Application

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献

    [1] Qiu P, et al. BMC Cancer. 2017, 17(1):55. [2] Fan YZ, et al. Hepatobiliary Pancreat Dis Int. 2010, 9(4):414

    合成参考文献


    摘要:Fan YZ, Zhao ZM, Fu JY, Chen CQ. [Anti-tumor mechanism of norcantharidin for the implanted tumors of human gallbladder carcinoma in nude mice in vivo]. Zhonghua Wai Ke Za Zhi. 2006 May 01;44(9):618–22.
    参考文献:10.3390/molecules19066911
    摘要:Wu JY, Kuo CD, Chu CY, Chen MS, Lin JH, Chen YJ, Liao HF. Synthesis of novel lipophilic N-substituted norcantharimide derivatives and evaluation of their anticancer activities. Molecules. 2014 May 26;19(6):6911–28.
    参考文献:10.1016/j.biopha.2018.04.100
    摘要:Chen F, Wang S, Wei Y, Wu J, Huang G, Chen J, Shi J, Xia J. Norcantharidin modulates the miR-30a/Metadherin/AKT signaling axis to suppress proliferation and metastasis of stromal tumor cells in giant cell tumor of bone. Biomed Pharmacother. 2018 Jul;103():1092–100. doi: 10.1016/j.biopha.2018.04.100.
    参考文献:10.1007/s11864-019-0663-0
    摘要:Majd N, Penas-Prado M. Updates on Management of Adult Medulloblastoma. Curr Treat Options Oncol. 2019 Jun 24;20(8):64. doi: 10.1007/s11864-019-0663-0.
    参考文献:10.3748/wjg.v27.i26.4203|10.3748/wjg.v27.i26.4208
    摘要:Li XY, Guan QX, Shang YZ, Wang YH, Lv SW, Yang ZX, Wang R, Feng YF, Li WN, Li YJ. Metal-organic framework IRMOFs coated with a temperature-sensitive gel delivering norcantharidin to treat liver cancer. World J Gastroenterol. 2021 Jul 14;27(26):4208–20.
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