CAS: 1355326-35-0; N-Cyclohexyl-2-(N-(3-Fluorophenyl)-2-(2-Methyl-1H-Imidazol-1-yl)Acetamido)-2-(O-Tolyl)Acetamide

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2-methylimidazole 2-chloro-N-(2-(cyclohexylamino)-2-oxo-1-(o-tolyl)ethyl)-N-(3-fluorophenyl)acetamide meta-fluoroaniline 2-methylphenyl aldehydeN-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-methyl-1H-imidazol-1-yl)acetamido)-2-(o-tolyl)acetamide hydr°Chloric acid

合成工艺路线路线简述

    3-氟苯胺置于三乙胺体系中,用 甲醇,二氯甲烷 用作溶剂,化学反应 4.0H,反应生成R132H-Idh1抑制剂(Agi-5198)
    参考文献:Discovery Of The First Potent Inhibitors Of Mutant Idh1 That Lower Tumor 2-Hg In Vivo
    标题:Discovery Of The First Potent Inhibitors Of Mutant Idh1 That Lower Tumor 2-Hg In Vivo
    摘要:Optimization Of A Series Of R132H Idh1 Inhibitors From A High Throughput Screen Led To The First Potent Molecules That Show Robust Tumor 2-Hg Inhibition In A Xenograft Model. Compound 35 Shows Good Potency In The U87 R132H Cell Based Assay And Similar To 90% Tumor 2-Hg Inhibition In The Corresponding Mouse Xenograft Model Following Bid Dosing. The Magnitude And Duration Of Tumor 2-Hg Inhibition Correlates With Free Plasma Concentration.
    Doi:10.1021/ml300225H

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    专利信息


    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: Chitneni SK, Reitman ZJ, Spicehandler R, Gooden DM, Yan H, Zalutsky MR. Synthesis and evaluation of radiolabeled AGI-5198 analogues as candidate radiotracers for imaging mutant IDH1 expression in tumors. Bioorg Med Chem Lett. 2018 Feb 15;28(4):694-699. doi: 10.1016/j.bmcl.2018.01.015. Epub 2018 Jan 12.
    2: Rohle D, Popovici-Muller J, Palaskas N, Turcan S, Grommes C, Campos C, Tsoi J, Clark O, Oldrini B, Komisopoulou E, Kunii K, Pedraza A, Schalm S, Silverman L, Miller A, Wang F, Yang H, Chen Y, Kernytsky A, Rosenblum MK, Liu W, Biller SA, Su SM, Brennan CW, Chan TA, Graeber TG, Yen KE, Mellinghoff IK. An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells. Science. 2013 May 3;340(6132):626-30. doi: 10.1126/science.1236062. Epub 2013 Apr 4.
    3: Molenaar RJ, Botman D, Smits MA, Hira VV, van Lith SA, Stap J, Henneman P, Khurshed M, Lenting K, Mul AN, Dimitrakopoulou D, van Drunen CM, Hoebe RA, Radivoyevitch T, Wilmink JW, Maciejewski JP, Vandertop WP, Leenders WP, Bleeker FE, van Noorden CJ. Radioprotection of IDH1-Mutated Cancer Cells by the IDH1-Mutant Inhibitor AGI-5198. Cancer Res. 2015 Nov 15;75(22):4790-802. doi: 10.1158/0008-5472.CAN-14-3603. Epub 2015 Sep 11. 29(9):1763-1782. doi: 10.1158/1078-0432.CCR-22-1896.

    合成参考文献


    参考文献:10.1016/j.bbamcr.2021.119114
    摘要:Bhattacharjee D, Balabhaskararao K, Jain N. Mutant IDH1 inhibitors activate pSTAT3-Y705 leading to an increase in BCAT1 and YKL-40 levels in mutant IDH1-expressing cells. Biochimica et Biophysica Acta (BBA) - Molecular Cell Research. 2021 Oct;1868(11):119114. doi: 10.1016/j.bbamcr.2021.119114.
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