CAS: 315183-21-2; N'-(3-Allyl-2-Hydroxybenzylidene)-2-(4-Benzylpiperazin-1-yl)Acetohydrazide

该化合物是一个小分子,在激活颗粒细胞方面起着重要作用,这种分子是进入potototologic 路径的肠胃癌的先质,其特点是能够选择性地激活丙草酮3-3,导致癌症细胞中的流行性硬化,使其成为肿瘤学的潜在治疗剂.PAC-1以其相对较低的分子量和具体的结构特征而著称,有利于其与胸腺相互作用.已经研究过它对于各种癌症细胞线的影响,表明它能够以依赖丙草酮的方式诱发细胞死亡.此外,PAC-1的行动机制包括稳定丙草酮3,促进将其转换为活性丙草酮-3形式.这一化合物对侧重于癌症治疗的研究感兴趣,特别是在提高现有疗法效率方面.然而,还需要进一步研究,以充分了解其药理学,潜在副作用和临床环境中的总体治疗潜力.

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CAS号24019-66-7 3-烯丙基-2-羟基苯甲醛 | CAS号24632-70-0 4-(苯甲基)-1-哌嗪乙酸

合成工艺路线路线简述

    📜1-苄基-4-(乙氧基羰基甲基)哌嗪置于盐酸,肼体系中,用 甲醇,乙醇,水 作为反应溶剂,化学反应 1.5H,反应生成 4-(苯基甲基)-1-哌嗪乙酸 2-[[2-羟基-3-(2-烯丙-1-基)苯基]亚甲基]酰肼
    参考文献:Wo2008/134474
    标题:Wo2008/134474

    海关参考信息

    专利信息


    专利号:US-7022730-B2
    优先权日:2001-10-19
    标题:Bis-heteroaryl alkanes as therapeutic agents
    发明人:MJALLI ADNAN M M; SHAHBAZ KATHY G J
    权利人:TRANSTECH PHARMA INC
    摘要:This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases in mammals mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.

    专利号:US-8916705-B2
    优先权日:2011-10-14
    标 题:Procaspase-activating compounds and compositions
    发明人:HERGENROTHER PAUL J
    权利人:UNIV ILLINOIS; TRUSTEES OF THE UNIVERSITY OF ILLILNOIS BOARD OF
    摘要:The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.

    专利号:EP-4058432-A1
    优先权日:2019-11-14
    标 题:Improved synthesis of kras g12c inhibitor compound

    专利号:US-9663482-B2
    优先权日:2012-08-03
    标 题:Substituted piperazinyl acetohydrazide procaspase-activating compounds
    发明人:HERGENROTHER PAUL J; ROTH HOWARD S
    权利人:UNIV ILLINOIS
    摘要:The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds are of Formula I n nThe compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.

    专利号:US-2014315915-A1
    优先权日:2009-02-09
    标题:Design, synthesis and evaluation of procaspase activating compounds as personalized anti-cancer drugs

    专利号:US-9522901-B2
    优先权日:2005-05-26
    标题:Compositions and methods including cell death inducers and procaspase activation
    发明人:HERGENROTHER PAUL J; PUTT KARSON S; PETERSON QUINN P; FAKO VALERIE
    权利人:UNIV ILLINOIS
    摘要:Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Inglott MA, Lerner EA, Pilowsky PM, Farnham MM. Activation of PAC(1) and VPAC receptor subtypes elicits differential physiological responses from sympathetic preganglionic neurons in the anaesthetized rat. Br J Pharmacol. 2012 Nov;167(5):1089-98. doi: 10.1111/j.1476-5381.2012.02045.x.
    2: Hsu DC, Roth HS, West DC, Botham RC, Novotny CJ, Schmid SC, Hergenrother PJ. Parallel synthesis and biological evaluation of 837 analogues of procaspase-activating compound 1 (PAC-1). ACS Comb Sci. 2012 Jan 9;14(1):44-50. doi: 10.1021/co2001372. Epub 2011 Oct 28.
    3: Zhang X, Tan F, Duan CZ. [Effect of electro-needling at acupoints of the yangming meridian on the expression of PAC-1 and lower limb functions in acute cerebral infarction patients]. Zhongguo Zhong Xi Yi Jie He Za Zhi. 2011 Apr;31(4):483-6. Chinese. doi: 10.1016/j.jpba.2010.07.042. Epub 2010 Aug 6. Chinese. doi: 10.1007/s10637-010-9445-z. Epub 2010 May 25.

    合成参考文献


    摘要:Li M, Cong Y, Deng X, Hu J, Qin X. [Impact of shear stress on expression of platelet membrane glycoproteins]. Zhonghua Yi Xue Za Zhi. 2002 Feb 25;82(4):267–70.
    参考文献:10.1158/0008-5472.can-03-3424
    摘要:Givant-Horwitz V, Davidson B, Reich R. Laminin-induced signaling in tumor cells: the role of the M(r) 67,000 laminin receptor. Cancer Res. 2004 May 15;64(10):3572–9. doi: 10.1158/0008-5472.can-03-3424.
    摘要:Angiolillo DJ, Fernandez-Ortiz A, Bernardo E, Ramírez C, Sabaté M, Hernández-Antolín R, Moreno R, Escaned J, Alfonso F, Bañuelos C, Macaya C. Is a 300 mg clopidogrel loading dose sufficient to inhibit platelet function early after coronary stenting A platelet function profile study. J Invasive Cardiol. 2004 Jun;16(6):325–9.
    参考文献:10.1136/pgmj.2006.047696
    摘要:Serebruany VL, Midei MG, Meilman H, Malinin AI, Lowry DR. Platelet inhibition with prasugrel (CS-747) compared with clopidogrel in patients undergoing coronary stenting: the subset from the JUMBO study. Postgrad Med J. 2006 Jun;82(968):404–10.
    参考文献:10.1111/j.1538-7836.2009.03716.x
    摘要:PENNINGS GJ, YONG ASC, KRITHARIDES L. Expression of EMMPRIN (CD147) on circulating platelets in vivo. Journal of Thrombosis and Haemostasis. 2010 Mar;8(3):472–81. doi: 10.1111/j.1538-7836.2009.03716.x.
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