Methyl 4beta-acetyloxy-3beta-hydroxy-16-methoxy-1-methyl-6,7-didehydro-2beta,5alpha,12beta,19alpha-aspidospermidine-3alpha-carboxylate

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 鸡蛋花型生物碱
• 英文名称: Methyl 4beta-acetyloxy-3beta-hydroxy-16-methoxy-1-methyl-6,7-didehydro-2beta,5alpha,12beta,19alpha-aspidospermidine-3alpha-carboxylate
• 英文别名: methyl (1S,9R,10S,11R,12R,19R)-11-acetyloxy-12-ethyl-10-hydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2(7),3,5,13-tetraene-10-carboxylate
• 化学式: C₂₅H₃₂N₂O₆
• 分子量: 456.5
• InChiKey: CXBGOBGJHGGWIE-IYJDUVQVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  88.5
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• [EN] A CONJUGATE OF A CYTOTOXIC AGENT TO A CELL BINDING MOLECULE WITH BRANCHED LINKERS<br/>[FR] CONJUGUÉ D'UN AGENT CYTOTOXIQUE À UNE MOLÉCULE DE LIAISON CELLULAIRE AVEC DES LIEURS RAMIFIÉS
  申请人：HANGZHOU DAC BIOTECH CO LTD

  公开号：WO2020257998A1

  公开（公告）日：2020-12-30

  Provided is a conjugation of cytotoxic drug to a cell-binding molecule with a side-chain linker. It provides side-chain linkage methods of making a conjugate of a cytotoxic molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and immunological disorders.

  提供了一种将细胞毒性药物与一个侧链连接分子结合的共轭物。它提供了制备细胞毒性分子与细胞结合配体的共轭物的侧链连接方法，以及在靶向治疗癌症、感染和免疫性疾病中使用该共轭物的方法。
• NOVEL VINBLASTINE DERIVATIVES, THEIR PREPARATION, USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAID DERIVATIVES
  申请人：Hu Lihong

  公开号：US20100113498A1

  公开（公告）日：2010-05-06

  The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors.

  该发明提供了以下式1所表示的长春碱衍生物或其生理上可接受的盐，它们的制备、用途以及包含所述衍生物的药物组合物。所述长春碱衍生物对肿瘤细胞系表现出抑制活性，可用作治疗恶性肿瘤的药物。
• COMPOSITIONS AND METHODS FOR TREATMENT OF VIRAL DISEASES
  申请人：Johansen Lisa M.

  公开号：US20100009970A1

  公开（公告）日：2010-01-14

  The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.

  本发明涉及用于治疗病毒性疾病的组合物、方法和试剂盒。在某些实施方式中，病毒性疾病是由单链RNA病毒、黄病毒科病毒或肝病毒引起的。在特定实施方式中，病毒性疾病是病毒性肝炎（例如甲型肝炎、乙型肝炎、丙型肝炎、丁型肝炎、戊型肝炎），药剂或药剂组合包括舍曲林、舍曲林类似物、UK-416244或UK-416244类似物。还包括用于鉴定可用于治疗病毒性疾病的新化合物的筛选方法。
• Process for the preparation of bisindole alkaloid derivatives
  申请人：Indena S.p.A.

  公开号：EP2135872A1

  公开（公告）日：2009-12-23

  A process for the coupling of catharantine and vindoline catalyzed by Laccases is described. The coupling produces anhydrovinblastine and anhydrovinblastine eniminium, which can be transformed to vinblastine or vinorelbine.

  描述了一种由漆酶催化的卡他兰丁和维诺啶偶联的过程。该偶联产生无水长春碱和无水长春碱亚胺，可以转化为长春碱或长春碱。
• Drug resistance and multidrug resistance modulators
  申请人：ELI LILLY AND COMPANY

  公开号：EP0844244A1

  公开（公告）日：1998-05-27

  Drug and multidrug resistant modulators of Formula (C): where Z is selected from the group consisting of -S-, -S(O)w-, and -CH2-, where w is 1 or 2; and pharmaceutically acceptable salts or solvates thereof are described and claimed.

  药物和多药耐药的调节剂的化学式（C）：其中Z选自由-S-，-S(O)w-和-CH2-组成的群，其中w为1或2；以及其药用可接受的盐或溶剂。