CAS: 56-25-7; Cantharidin

该化合物是一种自然形成的化学化合物,主要来自泡泡虫物种,特别是莱塔的这种物种;它是室内温度下无色,无味和粘粘液,水中沸点高,溶解度低,但有机溶剂中溶解性低; 甘沙里丁因其强大的植物特性而闻名,这意味着它会在接触时导致皮肤发泡; 该化合物历来用于传统医学,以达到其所谓的治疗效果,包括作为对蚊子和其他皮肤状况的治疗; 然而,它也因其毒性而得到承认,如果浸泡或处理不当,可能会造成严重的健康问题; 行动机制涉及蛋白磷酸的抑制,这扰乱了细胞过程; 由于其毒性性质,甘沙里丁在许多管辖区受到管制,其使用仅限于在专业监督下的具体医疗应用.

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CAS号75532-26-2 O,O-dimethyl ph... | CAS号75538-64-6 (5E,7Z)-dodeca-... | CAS号110-00-9 呋喃 | CAS号7647-01-0 盐酸 | CAS号853200-58-5 2-hydroxy-3a,7a... | CAS号95-47-6 邻二甲苯 | CAS号110-00-9 呋喃 | CAS号766-39-2 二甲基马来酸酐 | CAS号76970-77-9 hexahydro-3a,7a... | CAS号91877-87-1 3a,7a-dimethyl-...

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    专利号:US-2004242897-A1
    优先权日:2002-07-31
    标题 :Universal support media for synthesis of oligomeric compounds
    发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH
    摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

    专利号:WO-2004011474-A1
    优先权日:2002-07-31
    标题:Universal support media for synthesis of oligomeric compounds
    发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
    权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
    摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

    专利号:US-6653468-B1
    优先权日:2002-07-31
    标 题 :Universal support media for synthesis of oligomeric compounds
    发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH
    权利人:ISIS PHARMACEUTICALS INC
    摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

    专利号:US-12221452-B2
    优先权日:2017-10-04
    标题:Synthesis of cantharidin
    发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
    权利人:VERRICA PHARMACEUTICALS INC
    摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

    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.
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    主要参考文献


    1: Ren Y, Zhang SW, Xie ZH, Xu XM, Chen LL, Lou ZG, Weng GB, Yao XP. Cantharidin induces G2/M arrest and triggers apoptosis in renal cell carcinoma. Mol Med Rep. 2016 Dec;14(6):5614-5618. doi: 10.3892/mmr.2016.5963. Epub 2016 Nov 23. doi: 10.1111/imb.12198. Epub 2015 Nov 14. doi: 10.1016/j.fitote.2015.10.008. Epub 2015 Oct 22. doi: 10.1016/j.bcp.2016.03.011. Epub 2016 Mar 23.
    5: Hsia TC, Lin JH, Hsu SC, Tang NY, Lu HF, Wu SH, Lin JG, Chung JG. Cantharidin induces DNA damage and inhibits DNA repair-associated protein levels in NCI-H460 human lung cancer cells. Environ Toxicol. 2015 Sep;30(10):1135-43. doi: 10.1002/tox.21986. Epub 2014 Mar 17. doi: 10.3892/or.2016.4684. Epub 2016 Mar 17.
    8: Huang Y, Wang Z, Zha S, Wang Y, Jiang W, Liao Y, Song Z, Qi Z, Yin Y. De Novo Transcriptome and Expression Profile Analysis to Reveal Genes and Pathways Potentially Involved in Cantharidin Biosynthesis in the Blister Beetle Mylabris cichorii. PLoS One. 2016 Jan 11;11(1):e0146953. doi: 10.1371/journal.pone.0146953. eCollection 2016.

    合成参考文献


    参考文献:10.1124/mol.119.115964
    摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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