1-(3-Chlorophenyl)-2-sulfanylidene-3,5-dihydropyrrolo[3,2-c]pyridin-4-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: 1-(3-Chlorophenyl)-2-sulfanylidene-3,5-dihydropyrrolo[3,2-c]pyridin-4-one
• 英文别名: 1-(3-chlorophenyl)-2-sulfanylidene-3,5-dihydropyrrolo[3,2-c]pyridin-4-one
• 化学式: C₁₃H₉ClN₂OS
• 分子量: 276.74
• InChiKey: UDTZJQDTYRVDPP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  64.4
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• USE OF MYELOPEROXIDASE (MPO) INHIBITORS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF TO TREAT MULTIPLE SYSYEM ATROPHY (MSA) 938
  申请人：ASTRAZENECA AB

  公开号：US20140221400A1

  公开（公告）日：2014-08-07

  The present invention relates to the use of MPO inhibitors for the treatment of multiple system atrophy. The present invention also relates to the use of MPO inhibitors for the treatment of Huntington's disease. The present invention also relates to the use of MPO inhibitors for neuroprotection.
• [EN] USE OF MYELOPEROXIDASE (MPO) INHIBITORS FOR THE TREATMENT OF CHEMORESISTANT ACUTE MYELOID LEUKEMIA (AML)<br/>[FR] UTILISATION D'INHIBITEURS DE MYÉLOPEROXYDASE (MPO) POUR LE TRAITEMENT DE LA LEUCÉMIE MYÉLOÏDE AIGUË (LMA) CHIMIORÉSISTANTE
  申请人：INST NAT SANTE RECH MED

  公开号：WO2020021300A1

  公开（公告）日：2020-01-30

  Chemotherapy commonly alters cellular redox balance and increases the oxidative state. Recent studies have reported that chemoresistant cells have an increased reactive oxygen species (ROS) content in hematological malignancies. Here the inventors demonstrate that chemoresistant acute myeloid leukemia (AML) cells have a decreased level of mitochondrial and cytosolic ROS associated with an overexpression of myeloperoxidase (MPO), a heme protein that converts chloride and hydrogen peroxide to hypochlorous acid (HOC1). They also show that high MPO-expressing AML cells are less sensitive to AraC in vitro and in vivo. Targeting MPO expression and enzyme activity sensitizes to AraC treatment by triggering sustained oxidative stress in the high MPO expressing AML cells. Thus the present invention relates to use of myeloperoxidase (MPO) inhibitors for the treatment of chemoresistant acute myeloid leukemia (AML).