4-(1-adamantyl)phenyl acetate | 63013-56-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚酯
• 英文名称: 4-(1-adamantyl)phenyl acetate
• 英文别名: 1-(4-Acetoxyphenyl)-adamantan；[4-(1-adamantyl)phenyl] acetate
• CAS: 63013-56-9
• 化学式: C₁₈H₂₂O₂
• mdl: MFCD00194283
• 分子量: 270.371
• InChiKey: ARCROJYJJMBGNU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  2

安全信息

• 危险等级：
  IRRITANT

文献信息

• COMPOUNDS THAT INHIBIT HIF-1 ACTIVITY, THE METHOD FOR PREPARATION THEREOF AND THE PHARMACEUTICAL COMPOSITION CONTAINING THEM AS AN EFFECTIVE COMPONENT
  申请人：Lee Jung Joon

  公开号：US20090306078A1

  公开（公告）日：2009-12-10

  Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.

  本文披露了一种HIF-1抑制剂，其制备方法，以及包含其作为活性成分的药物组合物。该HIF-1抑制剂显示抗癌活性，这归功于其对HIF-1的抑制活性，HIF-1是一种在癌症生长和转移中起重要作用的转录因子，但不具有一般细胞毒性。因此，HIF抑制剂及其药用可接受的盐可用作治疗各种癌症，如肝癌、胃癌和乳腺癌的治疗药物。此外，具有对HIF-1抑制活性的化合物在治疗由HIF-1介导的VEGF表达加重的糖尿病视网膜病变和关节炎方面是有用的。
• ARYLOXY PHENOXY ACRYLIC COMPOUND HAVING HIF-1 INHIBITION ACTIVITY, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ACTIVE INGREDIENT
  申请人：Lee Kyeong

  公开号：US20130237542A1

  公开（公告）日：2013-09-12

  The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.

  本发明涉及一种抑制HF-1活性的化合物，以及该化合物的制备方法和包含该化合物作为活性成分的药物组合物。本发明的化合物通过抑制HIF-1活性而不是通过非选择性细胞毒性表现出抗癌活性，HIF-1是在癌细胞生长和转移中起重要作用的转录因子。因此，根据本发明的化合物或其药用盐抑制HIF-1活性，因此可以用作固体肿瘤如结肠癌、肝癌、胃癌和乳腺癌的治疗剂。此外，根据本发明的化合物或其药用盐还可以用作糖尿病视网膜病变或关节炎的治疗剂的活性成分，当HIF-1诱导的VEGF表达增加时，这些疾病可能会恶化。
• Small-Molecule Hydrophobic Tagging of Fusion Proteins and Induced Degradation of Same
  申请人：Yale University

  公开号：US20140302523A1

  公开（公告）日：2014-10-09

  The present invention includes compounds that are useful in perturbing or disrupting the function of a transmembrane or intracellular protein, whereby binding of a compound to the transmembrane or intracellular protein induces proteasomal degradation of the transmembrane or intracellular protein. The present invention further includes a method of inducing proteasomal degradation of a transmembrane or intracellular protein. The present invention further includes a method of identifying or validating a protein of interest as a therapeutic target for treatment of a disease state or condition.

  本发明包括一些化合物，这些化合物有助于扰乱或破坏跨膜或胞内蛋白的功能，其中化合物与跨膜或胞内蛋白的结合诱导跨膜或胞内蛋白的蛋白酶体降解。本发明还包括一种诱导跨膜或胞内蛋白的蛋白酶体降解的方法。本发明还包括一种鉴定或验证感兴趣蛋白作为治疗疾病状态或病情的治疗靶点的方法。
• Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same
  申请人：YALE UNIVERSITY

  公开号：US10145848B2

  公开（公告）日：2018-12-04

  The present invention includes compounds that are useful in perturbing or disrupting the function of a transmembrane or intracellular protein, whereby binding of the compounds to the transmembrane or intracellular protein induces proteasomal degradation of the transmembrane or intracellular protein. The present invention further includes a method of inducing proteasomal degradation of a transmembrane or intracellular protein. The present invention further includes a method of identifying or validating a protein of interest as a therapeutic target for treatment of a disease state or condition.

  本发明包括可用于扰乱或破坏跨膜或细胞内蛋白质功能的化合物，其中化合物与跨膜或细胞内蛋白质结合可诱导跨膜或细胞内蛋白质的蛋白酶体降解。本发明还包括一种诱导跨膜蛋白质或细胞内蛋白质的蛋白酶体降解的方法。本发明还包括一种鉴定或验证感兴趣的蛋白质作为治疗疾病状态或状况的治疗靶点的方法。
• SMALL-MOLECULE HYDROPHOBIC TAGGING OF FUSION PROTEINS AND INDUCED DEGRADATION OF SAME
  申请人：Yale University

  公开号：EP2649099A2

  公开（公告）日：2013-10-16