CAS: 12772-57-5; (1Ar,2Z,4E,14R,15Ar)-8-Chloro-1A,14,15,15A-Tetrahydro-9,11-Dihydroxy-14-Methyl-6H-Oxireno[e][2]Benzoxacyclotetradecin-6,12(7H)-Dione

该化合物是属于类化合物的天然产品,称为抗沙米素,主要被确认为具有耐热性抑制剂作用的热休克蛋白90(Hsp90),它对各种客户蛋白的正确折叠和功能至关重要,包括许多癌症病情发展过程; 放射物质呈现一种复杂的结构,具有双环核心和独特的侧链的特点,有助于其生物活动; 该化合物由于其潜在的治疗应用,特别是针对肿瘤细胞的治疗应用,已引起对药用化学和癌症研究的兴趣. 此外, 放射物质已表现出抗风素特性,使其与真菌感染研究相关. 它的行动机制涉及破坏Hsp90的守护器功能,导致客户蛋白质退化. 然而,为了充分了解其药理学特征和临床环境的潜在副作用,有必要进一步研究.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

CAS号75207-13-5 Mon°Cillin I | CAS号378749-88-3 (3R,4R,6S)-6-(h... | CAS号378750-02-8 (3R,4R,6S)-6-(t... | CAS号480-64-8 苔色酸 | CAS号867367-94-0 (R)-1-((2R,3R)-... | CAS号867367-83-7 (R)-1-((2R,3R)-... | CAS号754201-18-8 (1aR,2Z,4E,14R,... | CAS号754201-22-4 (1aR,2Z,4E,14R,...

合成工艺路线路线简述

    📜2,4-二羟基-6-甲基苯甲酸置于rucl2(1,3-Dimesityl-Imidazolidin-2-yl)(Pcy3)(=chph) 盐酸,磺酰氯,偶氮二甲酸二异丙酯,三(3-氯苯基)膦,双氧水,四丁基碘化铵,Potassium Carbonate,N,N-二异丙基乙胺,Lithium Diisopropyl Amide体系中,用 四氢呋喃,1,4-二氧六环,乙醚,N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 14.83H,反应生成根赤壳菌素
    参考文献:Radicicol(monorden)和pochonin C的溶液和固相合成.
    标题:Radicicol(monorden)和pochonin C的溶液和固相合成.
    摘要:报道了软骨素c和radicicol的模块化合成.两种天然产物分别从三个易得的片段中分七个步骤和八个步骤制备.这些化合物的替代合成是通过结合聚合物的试剂和固相反应实现的.研究了两种天然产物的构象,并通过2D NMR光谱进行了比较.
    Doi:10.1002/chem.200500160

    海关参考信息

    专利信息


    专利号:WO-2017100796-A1
    优先权日:2015-12-11
    标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
    权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.

    专利号:US-2017283878-A1
    优先权日:2015-12-11
    标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
    权利人:ACADEMIA SINICA
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

    专利号:US-2025206743-A1
    优先权日:2022-03-25
    标 题:Tyk2 inhibitor synthesis and intermediates thereof
    发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
    权利人:TAKEDA PHARMACEUTICALS CO
    摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

    专利号:US-9051302-B2
    优先权日:2008-01-15
    标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
    发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
    权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
    摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

    专利号:US-8314132-B2
    优先权日:2008-04-30
    标题:5-aryl-4-(5-substituted 2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone and the intermediates for production thereof
    发明人:MATULIS DAUMANTAS; CIKOTIENE INGA; KAZLAUSKAS EGIDIJUS; MATULIENE JURGITA
    权利人:MATULIS DAUMANTAS; CIKOTIENE INGA; KAZLAUSKAS EGIDIJUS; MATULIENE JURGITA; BIOTECHNOLOGIJOS INST
    摘要:Invention is related to novel compounds -5-aryl-4-(5-substituted 2,4-dihydroxyphenyl)-1,2,3-thiadiazoles with general formula (I). The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit Hsp90 chaperone which participate in cancer progression. This invention is also related to new intermediate compounds which are used for the synthesis of thiadiazoles of general formula (I).

    专利号:US-2025289827-A1
    优先权日:2022-12-02
    标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
    发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
    权利人:C4 THERAPEUTICS INC
    摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

    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: Liu Z, Lu Y, Tang D, Zhu J, Luo L, Chen Y, Yu H. Molecular Phylogenetic and Comparative Genomic Analysis of Pleurocordyceps fusiformispora sp. nov. and Perennicordyceps elaphomyceticola in the Family Polycephalomycetaceae. J Fungi (Basel). 2024 Apr 19;10(4):297. doi: 10.3390/jof10040297.
    2: da Silva CM, de Lima Neto RG, de Carvalho AMR, Macêdo DPC, de Azevedo Melo AS, Neves RP. Taxonomy of Candida parapsilosis complex isolated from neonates and the role of Hsp90 inhibitors to enhanced the antifungal activity of micafungin. Lett Appl Microbiol. 2024 May 3;77(5):ovae044. doi: 10.1093/lambio/ovae044.
    345:199379. doi: 10.1016/j.virusres.2024.199379. Epub 2024 Apr 26.

    合成参考文献


    参考文献:10.1021/ol052263+
    摘要:Moulin E, Barluenga S, Winssinger N. Concise synthesis of pochonin A, an HSP90 inhibitor. Org Lett. 2005 Dec 08;7(25):5637–9. doi: 10.1021/ol052263+.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知