CAS: 1010085-13-8; Trans-4-(3-Chloro-2-Fluorophenoxy)-1-((6-(Thiazol-2-Ylamino)Pyridin-2-yl)Methyl)Cyclohexane-1-Carboxylic Acid

该化合物是一种合成有机化合物,其特征是其复杂的分子结构,包括多种功能组.该化合物具有一种环氧乙酸混合物,表明存在一种有助于其酸性和潜在反应的碳箱酸功能组.一个碳箱酸环和一种丙烯衍生物的存在表明生物活动可能是一种药剂.氯氟苯氧化合物组增强了其亲性,这可能影响其在生物系统中的吸收和分布.此外,这种跨式结构还意味着特定的立体化学特性,可能影响其与生物目标的相互作用.

结构式图片

合成工艺路线路线简述

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    专利信息


    专利号:US-2022143183-A1
    优先权日:2019-02-23
    标题:Photoswitchable protacs and synthesis and uses thereof
    发明人:TRAUNER DIRK; REYNDERS MARTIN; MATSUURA BRYAN; BEROUTI MARLEEN; PAGANO MICHELE
    权利人:UNIV NEW YORK
    摘要:Provided are compounds, which may be referred to as PHOTACs (photoswitchable proteolysis targeting chimeras), and compositions, kits, and methods of making and using PHOTACs. PHOTACs have one or more E3 ligase ligand(s), one or more photoswitchable group(s), optionally, one or more linker(s), and one or more ligand(s) for a target protein. PHOTACs may be suitable for use in methods to treat diseases, such as, for example, cancer. PHOTACs may also be suitable for use in methods to induce selective degradation of a target protein.

    专利号:US-11285169-B2
    优先权日:2013-03-13
    标题 :Methods for modulating chemotherapeutic cytotoxicity
    发明人:ROBERTS DAVID D; SOTO PANTOJA DAVID R
    权利人:US HEALTH
    摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.
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    主要参考文献


    1: Jiang M, Bai M, Xu S, Wang T, Lei J, Xu M, Huang S, Jia Z, Zhang A. Blocking AURKA with MK-5108 attenuates renal fibrosis in chronic kidney disease. Biochim Biophys Acta Mol Basis Dis. 2021 Nov 1;1867(11):166227. doi: 10.1016/j.bbadis.2021.166227. Epub 2021 Jul 24. 23(9-10):492-511. doi: 10.1007/s10495-018-1472-9.
    3: Noronha S, Alt LAC, Scimeca TE, Zarou O, Obrzut J, Zanotti B, Hayward EA, Pillai A, Mathur S, Rojas J, Salamah R, Chandar N, Fay MJ. Preclinical evaluation of the Aurora kinase inhibitors AMG 900, AZD1152-HQPA, and MK-5108 on SW-872 and 93T449 human liposarcoma cells. In Vitro Cell Dev Biol Anim. 2018 Jan;54(1):71-84. doi: 10.1007/s11626-017-0208-4. Epub 2017 Dec 1. 34(1):84-95. doi: 10.1007/s10637-015-0306-7. Epub 2015 Dec 1.
    5: Chinn DC, Holland WS, Mack PC. Anticancer activity of the Aurora A kinase inhibitor MK-5108 in non-small-cell lung cancer (NSCLC) in vitro as monotherapy and in combination with chemotherapies. J Cancer Res Clin Oncol. 2014 Jul;140(7):1137-49. doi: 10.1007/s00432-014-1675-6. Epub 2014 Apr 23.

    合成参考文献


    摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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