庚二酸二(N-琥珀酰亚胺基)酯 | 74648-14-9

• 物质功能分类: 医药中间体 - 杂环化合物
• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 庚二酸二(N-琥珀酰亚胺基)酯
• 英文名称: pimelic acid dihydroxysuccinimide ester
• 英文别名: 1,1'-[(1,7-dioxoheptane-1,7-diyl)bis(oxy)]dipyrrolidine-2,5-dione；bis(2,5-dioxopyrrolidin-1-yl) heptanedioate；1-({7-[(2,5-dioxo-1-pyrrolidinyl)oxy]-7-oxoheptanoyl}-oxy)-2,5-pyrrolidine-dione
• CAS: 74648-14-9
• 化学式: C₁₅H₁₈N₂O₈
• 分子量: 354.317
• InChiKey: LOJVONPJBWABIQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  25
• 可旋转键数：
  10
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  127
• 氢给体数：
  0
• 氢受体数：
  8

安全信息

• 危险性防范说明：
  P264,P280,P302+P352,P337+P313,P305+P351+P338,P362+P364,P332+P313
• 危险性描述：
  H315,H319

反应信息

• 作为反应物：
  描述：

  庚二酸二(N-琥珀酰亚胺基)酯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 52.0h， 生成 heptanedioic acid (4-methoxyphenyl)amide (2-oxotetrahydrofuran-3-yl)amide
  参考文献：
  名称：

  Antibody Interference with N-Acyl Homoserine Lactone-Mediated Bacterial Quorum Sensing

  摘要：

  Many bacterial pathogens coordinate their virulence factor expression in a cell density-dependent manner. This population-dependent coordination of gene expression in bacteria has been termed "quorum sensing" (QS). N-Acyl homoserine lactones (AHLs) are used by over 70 Gram-negative bacterial species as autoinducers. Inhibition of QS signaling might represent a new target for antimicrobial therapy. Here we report the hapten design, synthesis, generation of monoclonal antibodies (mAbs) against AHLs, and the evaluation of these mAbs for their ability to blunt QS signaling and inhibit virulence factor expression in P. aeruginosa. The mAbs can be envisioned as a tool for future investigations into AHL-based QS, which may aid in gaining new insights into the pathogenesis of P. aeruginosa and may ultimately lead to the development of new strategies to combat bacterial diseases.

  DOI：

  10.1021/ja0578698
• 作为产物：
  描述：

  N-羟基丁二酰亚胺 、 1,7-庚二酰氯 在 三乙胺 作用下， 以 四氢呋喃 为溶剂， 以90%的产率得到庚二酸二(N-琥珀酰亚胺基)酯
  参考文献：
  名称：

  DNA结合酰胺连接的双插联双蒽并吡唑类抗癌化合物的基于结构的设计，合成和生物学评估

  摘要：

  一系列酰胺偶联的7-氯-2- [2-[（[2-羟乙基）甲基氨基]乙基]蒽[1,9 - cd ]吡唑-6（2 H）的联蒽并吡唑衍生物使用分子建模和对接设计一个（AP9）并合成，以开发一种抗癌药物，该药物与DNA形成强结合双嵌入复合物。DNA融解温度升高的浓度依赖性用于确定DNA结合强度以及新合成的类似物是否发生双嵌入。还测量了化合物抑制人红白血病K562细胞系生长和抑制DNA拓扑异构酶IIα的脱级活性的能力。最后，通过测量拓扑异构酶IIα介导的DNA双链切割，评估了这些化合物作为拓扑异构酶II毒物的能力。所有的双蒽吡唑均在低微摩尔范围内抑制K562细胞的生长和拓扑异构酶IIα。具有两个或三个亚甲基接头的化合物与DNA形成双插层络合物，并与阿霉素一样强或更强地结合。总之，设计，合成了一组新的酰胺偶联双插入蒽吡唑化合物，并评估了其作为潜在抗癌剂的理化和生物学特性。

  DOI：

  10.1016/j.bmc.2009.04.072

文献信息

• [EN] SPLICEOSTATIN ANALOGS<br/>[FR] ANALOGUES DE SPLICÉOSTATINE
  申请人：PFIZER

  公开号：WO2014068443A1

  公开（公告）日：2014-05-08

  The present invention is directed to novel cytotoxic spliceostatin analogs (I) and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.

  本发明涉及新型细胞毒性剪接抑制素类似物（I）及其衍生物，涉及其抗体药物结合物，以及使用它们治疗包括癌症在内的医疗状况的方法。
• Preparation of fluorescence-labeled and cross-linked subtilisin.
  作者：Kazutaka TANIZAWA、Tsutomu MANO、Yuichi KANAOKA

  DOI：10.1248/cpb.38.464

  日期：——

  Streptomyces subtilisin inhibitor (SSI) is a protein characterized by both its potent inhibitory activity toward subtilisin and its structure, composed of two homologous subunits. It binds two molecules of subtilisin to form a tetrameric complex.Intermolecularly cross-linked subtilisin is expected to form a polymeric complex with SSI. This could provide a useful model of protein-protein associatin. Therefore, Preparation of fluorescence-labeled and cross-linked subtilisin was carried out.

  链霉菌亚硫蛋白酶抑制剂（SSI）是一种蛋白质，具有对亚硫蛋白酶的强抑制活性，并且其结构由两个同源亚基组成。它能结合两个亚硫蛋白酶分子形成四聚体复合物。通过分子间交联的亚硫蛋白酶预计将与SSI形成聚合复合物。这可以提供一个有用的蛋白质-蛋白质结合模型。因此，进行了荧光标记和交联亚硫蛋白酶的制备。
• [EN] ERIBULIN-BASED ANTIBODY-DRUG CONJUGATES AND METHODS OF USE<br/>[FR] CONJUGUÉS ANTICORPS-MÉDICAMENT À BASE D'ÉRIBULINE ET LEURS PROCÉDÉS D'UTILISATION
  申请人：EISAI INC

  公开号：WO2017151979A1

  公开（公告）日：2017-09-08

  Linker toxins and antibody-drug conjugates that bind to human oncology antigen targets such as folate receptor alpha and/or provide anti-tubulin drug activity are disclosed. The linker toxins and antibody-drug conjugates comprise an eribulin drug moiety and can be internalized into target antigen-expressing cells. The disclosure further relates to methods and compositions for use in the treatment of cancer by administering the antibody-drug conjugates provided herein.

  本文揭示了与人体肿瘤抗原靶点如叶酸受体α结合并/或提供抗微管药物活性的连接毒素和抗体药物结合物。这些连接毒素和抗体药物结合物包括依立必利药物部分，并且可以被内化到表达目标抗原的细胞内。该公开还涉及通过给予本文提供的抗体药物结合物来治疗癌症的方法和组合物。
• SPLICEOSTATIN ANALOGS AND METHODS FOR THEIR PREPARATION
  申请人：PFIZER INC.

  公开号：US20140134193A1

  公开（公告）日：2014-05-15

  The present invention is directed to novel cytotoxic spliceostatin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.

  本发明涉及新型细胞毒性剪接素类似物和衍生物，其抗体药物偶联物，以及使用它们治疗包括癌症在内的医学状况的方法。
• CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTICS DELIVERY
  申请人：Cerulean Pharma Inc.

  公开号：US20130129665A1

  公开（公告）日：2013-05-23

  The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

  本发明涉及一种新型的治疗环糊精聚合物组合物，设计为小分子治疗药物的载体，以及其制药组合物。这些含环糊精的聚合物提高了药物的稳定性和溶解性，并在体内使用时降低了小分子治疗药物的毒性。此外，通过从各种连接基团和靶向配体中选择，这些聚合物呈现出治疗剂的可控释放方法。本发明还涉及使用所述治疗组合物治疗受试者的方法。本发明还涉及用于进行制药业务的方法，包括制造、许可或分发包含或涉及所述聚合物化合物的工具箱。