6-O-trityl-d-glucose

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: 6-O-trityl-d-glucose
• 英文别名: 6-O-trityl glucose；(2R,3S,4R,5R)-2,3,4,5-Tetrahydroxy-6-(trityloxy)hexanal；(2R,3S,4R,5R)-2,3,4,5-tetrahydroxy-6-trityloxyhexanal
• 化学式: C₂₅H₂₆O₆
• 分子量: 422.478
• InChiKey: QHDZNFSMOJVIIL-OLKYXYMISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  31
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  107
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  6-O-trityl-d-glucose 在 甲醇 、 sodium tetrahydroborate 作用下， 生成 6-O-trityl-D-sorbitol
  参考文献：
  名称：

  喜树碱偶联分子载体的制备及其对人大肠癌的细胞毒作用

  摘要：

  喜树碱（CPT）及其衍生物是唯一针对DNA拓扑异构酶I的酶活性的化学类别，该酶活性涉及DNA损伤和随后的细胞凋亡。尽管CPT具有许多优点，但由于其极差的溶解度，多个外排泵的耐药性，半衰期短和生物利用度差等原因，其使用受到了限制。为了克服这些局限性，我们设计并合成了一种水溶性CPT偶联分子转运蛋白，该分子转运蛋白可将CPT成功快速地传递到细胞中。该缀合物对细胞内部的线粒体具有亲和力，并且主要分布于肾脏，肺和脾脏。MTT分析证实，CPP偶联物比结肠癌药物可大大降低结肠癌细胞系的细胞活力。体内应用，特别是用于结肠癌的治疗。

  DOI：

  10.1002/bkcs.11611
• 作为产物：
  描述：

  a-无水葡萄糖酯 、 三苯基氯甲烷 在 吡啶 作用下， 生成 6-O-trityl-d-glucose
  参考文献：
  名称：

  喜树碱偶联分子载体的制备及其对人大肠癌的细胞毒作用

  摘要：

  喜树碱（CPT）及其衍生物是唯一针对DNA拓扑异构酶I的酶活性的化学类别，该酶活性涉及DNA损伤和随后的细胞凋亡。尽管CPT具有许多优点，但由于其极差的溶解度，多个外排泵的耐药性，半衰期短和生物利用度差等原因，其使用受到了限制。为了克服这些局限性，我们设计并合成了一种水溶性CPT偶联分子转运蛋白，该分子转运蛋白可将CPT成功快速地传递到细胞中。该缀合物对细胞内部的线粒体具有亲和力，并且主要分布于肾脏，肺和脾脏。MTT分析证实，CPP偶联物比结肠癌药物可大大降低结肠癌细胞系的细胞活力。体内应用，特别是用于结肠癌的治疗。

  DOI：

  10.1002/bkcs.11611

文献信息

• Methods for manufacturing polysaccharide derivatives
  申请人：——

  公开号：US20040137582A1

  公开（公告）日：2004-07-15

  The invention is based upon the discovery that insoluble, polysaccharides, such as inulin and dextran, can be enzymatically modified in an organic solvent. Thus, the invention relates to methods for making a high molecular weight polyhydroxy polymer, such as a polysaccharide, inulin or dextran derivative, comprising reacting an acyl donor and the polymer, such as inulin or dextran, to form an acyl ester of the polymer, such as inulin dextran, in a reaction medium comprising an organic solvent in the presence of a hydrolytic enzyme; methods for making a polymer, such as a polysaccharide, an inulin or dextran polymer, comprising reacting a polymerizable acyl donor and polyhydroxyl polymer in a reaction medium comprising an organic solvent in the presence of a hydrolytic enzyme thereby making an polymeric monomer, such as an inulin monomer, and polymerizing, preferably dimerizing, the monomer, thereby making a novel polymer, such as an inulin polymer. The invention further relates to novel products as can be produced by the processes described herein, pharmaceutical compositions containing them and the use of the novel polymers described herein in methods for the manufacture of a pharmaceutical composition or medicament. Further, the invention relates to a method of delivering an active agent to a patient comprising administering to the patient a pharmaceutical composition described herein.

  本发明的基础是发现菊粉和葡聚糖等不溶性多糖可以在有机溶剂中进行酶改性。因此，本发明涉及制造高分子量多羟基聚合物（如多糖、菊粉或葡聚糖衍生物）的方法，包括在水解酶存在下，在包括有机溶剂的反应介质中，使酰基供体与聚合物（如菊粉或葡聚糖）反应，形成聚合物（如菊粉葡聚糖）的酰基酯；制造聚合物，如多糖、菊粉或葡聚糖聚合物的方法，包括在水解酶存在下，在包含有机溶剂的反应介质中，使可聚合酰基供体和多羟基聚合物反应，从而制得聚合物单体，如菊粉单体，并使单体聚合，最好是二聚，从而制得新型聚合物，如菊粉聚合物。本发明进一步涉及可通过本文所述工艺生产的新型产品、含有这些产品的药物组合物以及本文所述新型聚合物在药物组合物或药物制造方法中的使用。此外，本发明还涉及一种向患者施用活性剂的方法，包括向患者施用本文所述的药物组合物。
• [EN] METHODS FOR MANUFACTURING POLYSACCHARIDE DERIVATIVES<br/>[FR] PROCEDES DE FABRICATION DE DERIVES DE POLYSACCHARIDE
  申请人：RENSSELAER POLYTECH INST

  公开号：WO2004024774A2

  公开（公告）日：2004-03-25

  The invention is based upon the discovery that insoluble, polysaccharides, such as inulin and dextran, can be enzymatically modified in an organic solvent. Thus, the invention relates to methods for making a high molecular weight polyhydroxy polymer, such as a polysaccharide, inulin or dextran derivative, comprising reacting an acyl donor and the polymer, such as inulin or dextran, to form an acyl ester of the polymer, such as inulin dextran, in a reaction medium comprising an organic solvent in the presence of a hydrolytic enzyme; methods for making a polymer, such as a polysaccharide, an inulin or dextran polymer, comprising reacting a polymerizable acyl donor and polyhydroxyl polymer in a reaction medium comprising an organic solvent in the presence of a hydrolytic enzyme thereby making an polymeric monomer, such as an inulin monomer, and polymerizing, preferably dimerizing, the monomer, thereby making a novel polymer, such as an inulin polymer. The invention further relates to novel products as can be produced by the processes described herein, pharmaceutical compositions containing them and the use of the novel polymers described herein in methods for the manufacture of a pharmaceutical composition or medicament. Further, the invention relates to a method of delivering an active agent to a patient comprising administering to the patient a pharmaceutical composition described herein.
• Preparation of a Camptothecin‐conjugated Molecular Carrier and its Cytotoxic Effect Toward Human Colorectal Carcinoma <i>In Vitro</i>
  作者：Dongjun Jeong、Tarun Pal、Hyungjoo Kim、Tae Wan Kim、Goutam Biswas、Daeun Lee、Tejinder Singh、Akula S. N. Murthy、Wanil Kim、Kyong‐Tai Kim、Jungkyun Im

  DOI：10.1002/bkcs.11611

  日期：2018.12

  designed and synthesized a water‐soluble CPT‐conjugated molecular transporter that successfully and rapidly delivered CPT into cells. The conjugate had affinity toward mitochondria inside cells and it was distributed mainly to kidney, lung, and spleen. MTT assay confirmed that the CPP‐conjugate decreased cell viability of colon cancer cell lines to a much greater extent than the parent drug. This novel

  喜树碱（CPT）及其衍生物是唯一针对DNA拓扑异构酶I的酶活性的化学类别，该酶活性涉及DNA损伤和随后的细胞凋亡。尽管CPT具有许多优点，但由于其极差的溶解度，多个外排泵的耐药性，半衰期短和生物利用度差等原因，其使用受到了限制。为了克服这些局限性，我们设计并合成了一种水溶性CPT偶联分子转运蛋白，该分子转运蛋白可将CPT成功快速地传递到细胞中。该缀合物对细胞内部的线粒体具有亲和力，并且主要分布于肾脏，肺和脾脏。MTT分析证实，CPP偶联物比结肠癌药物可大大降低结肠癌细胞系的细胞活力。体内应用，特别是用于结肠癌的治疗。