2-[4-[(4R,5S)-4,5-bis(4-chlorophenyl)-2-(2-ethoxyphenyl)imidazolidine-2-carbonyl]piperazin-1-yl]acetaldehyde

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: 2-[4-[(4R,5S)-4,5-bis(4-chlorophenyl)-2-(2-ethoxyphenyl)imidazolidine-2-carbonyl]piperazin-1-yl]acetaldehyde
• 化学式: C₃₀H₃₂Cl₂N₄O₃
• 分子量: 567.5
• InChiKey: YUVDQSMTDHPUQH-SCPSXFHPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  39
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  73.9
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• INHIBITION OF PULMONARY FIBROSIS WITH NUTLIN-3A AND PEPTIDES
  申请人：Board of Regents, The University of Texas System

  公开号：EP2970383A1

  公开（公告）日：2016-01-20
• [EN] INHIBITION OF PULMONARY FIBROSIS WITH NUTLIN-3A AND PEPTIDES<br/>[FR] INHIBITION DE LA FIBROSE PULMONAIRE PAR LA NUTLIN-3A ET DES PEPTIDES
  申请人：UNIV TEXAS

  公开号：WO2014145389A1

  公开（公告）日：2014-09-18

  In fibrotic lung fibroblasts, basal levels of p53 protein (and miR-34a) are markedly suppressed, leading to reduced p53-mediated inhibition of uPA and uPAR, or concurrent induction of PAI-1. These changes contribute to excessive FL-fibroblast proliferation and production of extracellular matrix (ECM), and, therefore, pulmonary fibrosis. These processes are reversed by treating the cells, and treating subjects suffering from idiopathic pulmonary fibrosis (IPF) with the small organic molecule nutlin-3a (NTL) or with a peptide, CSP-4 (SEQ ID NO:1), or variants or derivatives or multimers of this peptide, which increase p53 levels by inhibiting MDM2-mediated degradation of p53 protein. Use of these compounds serves as a new approach to the treatment of IPF, as they restore p53 expression and p53-mediated changes in the uPA-fibrinolytic system in FL-fibroblasts and restrict production and deposition of ECM.