(-)-Stellettin E

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 英文名称: (-)-Stellettin E
• 英文别名: (2E,4E,6E,8E,10Z)-10-[(3aS,5aR,9aR,9bS)-3a,6,6,9a-tetramethyl-2,7-dioxo-4,5,5a,8,9,9b-hexahydro-1H-cyclopenta[a]naphthalen-3-ylidene]-2,6-dimethylundeca-2,4,6,8-tetraenoic acid
• 化学式: C₃₀H₄₀O₄
• 分子量: 464.6
• InChiKey: IIPLLKSCMYHUOP-HJMNRKRYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.1
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  71.4
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• OSW-1 ANALOGS AND CONJUGATES, AND USES THEREOF
  申请人：Shair Matthew D.

  公开号：US20140135279A1

  公开（公告）日：2014-05-15

  Provided are a number of compounds structurally related to OSW-1, a natural compound that binds OSBPs. Also provided are pharmaceutical compositions comprising the OSW-1 analogs, as well as methods for use of these OSW-1 analogs, or pharmaceutically acceptable salts, enantiomers, or stereoisomers thereof in the treatment of atherosclerosis. Alzheimer's disease, and cancer, including p21-deficient cancer. Conjugates of OSW-1 analogs with monoclonal antibodies, including monoclonal antibodies targeted to cancer cells, are also provided. Also provided are pharmaceutical compositions comprising the conjugates, as well as methods for use of these conjugates, in the treatment of cancer, including p21-deficient cancer.

  提供了一些结构与OSW-1相似的化合物，OSW-1是一种与OSBPs结合的天然化合物。还提供了包含OSW-1类似物的制药组合物，以及使用这些OSW-1类似物或其药学上可接受的盐、对映体或立体异构体治疗动脉粥样硬化、阿尔茨海默病和癌症，包括p21缺陷癌症的方法。还提供了与单克隆抗体结合的OSW-1类似物共轭物，包括针对癌细胞的单克隆抗体。还提供了包含这些共轭物的制药组合物，以及使用这些共轭物治疗癌症，包括p21缺陷癌症的方法。
• Compounds That Bind Oxysterol Binding Proteins, and Methods of Use Thereof
  申请人：Shair Matthew D.

  公开号：US20110319352A1

  公开（公告）日：2011-12-29

  The invention relates in part to the discovery that certain CRAMs, such as schweinfurthin A, target OSBPs (a family of oxysterol binding proteins). Because OSBPs have been shown to be integral to atherosclerosis and Alzheimer's disease (AD), one aspect of the invention relates to the use of CRAMs, or a pharmaceutically acceptable salt, biologically active metabolite, solvate, hydrate, prodrug, enantiomer or stereoisomer thereof, in the treatment and/or prevention of atherosclerosis, Alzheimer's disease and related disorders. Another aspect of the invention relates to novel derivatives of CRAMs, or a pharmaceutically acceptable salt, biologically active metabolite, solvate, hydrate, prodrug, enantiomer or stereoisomer thereof, for the treatment and/or prevention of atherosclerosis, Alzheimer's disease and related disorders. Another aspect of the invention relates to the use of an immobilized CRAMs, such as OSW-I, to aid in screening of compounds to identify additional OSBP binders. Other aspects of the invention relate to the use of CRAMs to treat cancer, such as p21-deficient cancers.
• US9790253B2
  申请人：——

  公开号：US9790253B2

  公开（公告）日：2017-10-17
• [EN] COMPOUNDS THAT BIND OXYSTEROL BINDING PROTEINS, AND METHODS OF USE THEREOF<br/>[FR] COMPOSITIONS SE LIANT À DES PROTÉINES DE LIAISON AVEC L'OXYSTÉROL, ET LEURS MÉTHODES D'UTILISATION
  申请人：HARVARD COLLEGE

  公开号：WO2010068877A2

  公开（公告）日：2010-06-17

  The invention relates in part to the discovery that certain CRAMs, such as schweinfurthin A, target OSBPs (a family of oxysterol binding proteins). Because OSBPs have been shown to be integral to atherosclerosis and Alzheimer's disease (AD), one aspect of the invention relates to the use of CRAMs, or a pharmaceutically acceptable salt, biologically active metabolite, solvate, hydrate, prodrug, enantiomer or stereoisomer thereof, in the treatment and/or prevention of atherosclerosis, Alzheimer's disease and related disorders. Another aspect of the invention relates to novel derivatives of CRAMs, or a pharmaceutically acceptable salt, biologically active metabolite, solvate, hydrate, prodrug, enantiomer or stereoisomer thereof, for the treatment and/or prevention of atherosclerosis, Alzheimer's disease and related disorders. Another aspect of the invention relates to the use of an immobilized CRAMs, such as OSW-I, to aid in screening of compounds to identify additional OSBP binders. Other aspects of the invention relate to the use of CRAMs to treat cancer, such as p21-deficient cancers.
• [EN] OSW-1 ANALOGS AND CONJUGATES, AND USES THEREOF<br/>[FR] CONJUGUÉS ET ANALOGUES D'OSW-1, ET LEURS UTILISATIONS
  申请人：HARVARD COLLEGE

  公开号：WO2012159027A2

  公开（公告）日：2012-11-22

  Provided are a number of compounds structurally related to OSW-1, a natural compound that binds OSBPs. Also provided are pharmaceutical compositions comprising the OSW-1 analogs, as well as methods for use of these OSW-1 analogs, or pharmaceutically acceptable salts, enantiomers, or stereoisomers thereof, in the treatment of atherosclerosis, Alzheimer's disease, and cancer, including p21 -deficient cancer. Conjugates of OSW-1 analogs with monoclonal antibodies, including monoclonal antibodies targeted to cancer cells, are also provided. Also provided are pharmaceutical compositions comprising the conjugates, as well as methods for use of these conjugates, in the treatment of cancer, including p21 -deficient cancer.