CAS: 121584-18-7; Valspodar

该化合物是P-glycoprotein (P-gp) 半脂泵的强大抑制剂,该泵在癌症治疗中的多种药物抗药性方面起着重要作用,被归类为一种非细胞毒性化合物,主要用于研究环境,通过防止各种抗癌药物被从癌症细胞中排出,提高这些药物的功效.Valspodar 展示了一种复杂的结构,包括多种芳香环,有助于其亲热性和跨细胞膜的能力.该化合物已被研究过,以了解其有可能提高乳胶化剂的药理学,从而提高其细胞内浓度和治疗效力.此外,Valspodar在临床试验中,特别是与其他药物一起,接受了评估其克服肿瘤抗药性机制的能力.在癌症治疗中,其安全特征和与其他药物的相互作用是一个重要的考虑因素.总的来说,Valspodar是当前在防治癌症抗药性方面进行的努力的一个重要领域.

结构式图片

合成工艺路线路线简述

    📜,二氯乙酸置于二氯乙酸体系中,用54的收率获得戊司泊达; 伐司扑达
    参考文献:Cyclosporins And Their Use As Pharmaceuticals
    标题:Cyclosporins And Their Use As Pharmaceuticals
    摘要:环孢霉素中,1-位置上的残基(通常为-Mebmt-或-Dihydro-Mebmt-)是3'O-酰化或3'-氧化或-C.Sub.1-4烷氧基亚胺取代的,或者2-位置上的残基是β-O-酰基或β-氧代取代的,或者2-位置上的残基是-Ile-,或者11-位置上的残基是-Meals-,-Meile-或-Mealloile-以及各种天然存在的环孢霉素/二氢衍生物,在逆转化疗药物抵抗性方面有用,特别是对细胞毒性或抗肿瘤治疗的抵抗性.其中的一些环孢霉素和其生产的中间体是新颖的.在1-位置上的残基(例如-Mebmt-,-Dihydro-Mebmt-等)为8'-烷氧基或7'-去甲基-7'-羟基烷基取代的中间体是新颖的,并且作为免疫抑制剂,抗炎和抗寄生虫剂是有用的.

    海关参考信息

    专利信息


    专利号:US-12391691-B2
    优先权日:2018-11-16
    标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
    发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
    权利人:AMGEN INC
    摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

    专利号:US-2006014987-A1
    优先权日:2003-07-07
    标 题:Synthesis of beta-elemene, intermediates thereto, analogues and uses thereof
    发明人:HUANG LAN
    权利人:HUANG LAN
    摘要:The present invention provides convergent processes for preparing beta-elemene, and analogues thereof. Also provided are analogues related to beta-elemene and intermediates useful for preparing the same. The present invention further provides novel compositions based on analogues of beta-elemene and methods for the treatment of cancer, such as brain tumor, lung cancer, colorectal cancer, gastric intestional cancer, and stomach cancer.

    专利号:US-2025241876-A1
    优先权日:2023-07-19
    标 题:Anti-tumor compounds and methods of use thereof and synthesis thereof
    发明人:QUAY STEVEN CARL
    权利人:ATOSSA THERAPEUTICS INC
    摘要:Described herein are pharmaceutical compounds and compositions and methods of making thereof. Methods of synthesis for the compounds are described herein. The compounds or compositions described herein may exhibit aromatase inhibition activity or estrogen receptor activity. The compounds and compositions described herein may be useful in the treatment of a condition in a subject.

    专利号:US-2023192682-A1
    优先权日:2019-11-14
    标题:Improved synthesis of kras g12c inhibitor compound

    专利号:US-2023192681-A1
    优先权日:2019-11-14
    标 题 :Improved synthesis of kras g12c inhibitor compound

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    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: Vig S, Srivastava P, Rahman I, Jaranson R, Dasgupta A, Perttilä R, Uusimaa P, Huang HC. Screening of photosensitizers-ATP binding cassette (ABC) transporter interactions in vitro. Cancer Drug Resist. 2024 Sep 21;7:35. doi: 10.20517/cdr.2024.50.
    2: Johnston CU, Kennedy CJ. Potency and mechanism of p-glycoprotein chemosensitizers in rainbow trout (Oncorhynchus mykiss) hepatocytes. Fish Physiol Biochem. 2024 Dec;50(6):2149-2164. doi: 10.1007/s10695-024-01376-9. Epub 2024 Jul 19. 54(6):342-349. doi: 10.1080/00498254.2024.2358395. Epub 2024 Jun 24.
    4: Piska K, Koczurkiewicz-Adamczyk P, Jamrozik M, Bucki A, Kołaczkowski M, Pękala E. Comparative study on ABCB1-dependent efflux of anthracyclines and their metabolites: consequences for cancer resistance. Xenobiotica. 2023 Dec;53(6-7):507-514. doi: 10.1080/00498254.2023.2264391. Epub 2023 Nov 3. 114(2):446-458. doi: 10.1002/cpt.2964. Epub 2023 Jul 3. 46(8):353-359. doi: 10.1097/COC.0000000000001014. Epub 2023 Jun 2.

    合成参考文献


    参考文献:10.1007/s10549-005-9026-6
    摘要:Villeneuve DJ, Hembruff SL, Veitch Z, Cecchetto M, Dew WA, Parissenti AM. cDNA microarray analysis of isogenic paclitaxel- and doxorubicin-resistant breast tumor cell lines reveals distinct drug-specific genetic signatures of resistance. Breast Cancer Research and Treatment. 2005 Dec 02;96(1):17–39. doi: 10.1007/s10549-005-9026-6.
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