SU6657 | 288144-21-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: SU6657
• 英文别名: Indolin-2-one deriv. 4c；(3Z)-2-oxo-3-(4,5,6,7-tetrahydro-1H-indol-2-ylmethylidene)-1H-indole-5-sulfonamide
• CAS: 288144-21-8
• 化学式: C₁₇H₁₇N₃O₃S
• 分子量: 343.406
• InChiKey: FHSRUXRMSRJDQV-ZSOIEALJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  24
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  113
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  4,5,6,7-四氢吲哚 在 哌啶 、 三氯氧磷 作用下， 以 乙醇 、 二氯甲烷 为溶剂， 反应 1.0h， 生成 SU6657
  参考文献：
  名称：

  Identification of Substituted 3-[(4,5,6,7-Tetrahydro-1H-indol-2-yl)methylene]- 1,3-dihydroindol-2-ones as Growth Factor Receptor Inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rβ Tyrosine Kinases

  摘要：

  A series of new 3-substituted indolin-2-ones containing a tetrahydroindole moiety was developed as specific inhibitors of receptor tyrosine kinases associated with VEGF-R, FGF-R, and PDGF-R growth factor receptors. These compounds were evaluated for their inhibitory properties toward VEGF-R2 (Flk-1/KDR), FGF-R1, PDGF-R beta, p60(c-Src), and EGF-R tyrosine kinases and their ability to inhibit growth factor-dependent cell proliferation. Structure-activity relationships of this new pharmacophore have been determined at the level of kinase inhibition. Compounds containing a propionic acid moiety at the C-3' position of the tetrahydroindole ring represented the most potent indolin-2-ones to inactivate the VEGF, FGF, and PDGF receptor kinases. The inhibitory activities of 9d against VEGF-R2 (Flk-1), 9h against FGF-R1, and 9b against PDGF-R beta were 4, 80, and 4 nM, respectively. However, all of these compounds were inactive when tested against the EGF-R tyrosine kinase. Compounds 9a and 9b represented the most potent inhibitors of these classes to inhibit both biochemical kinase and growth factor-dependent cell proliferation for these three targets. In addition, compound 9a was cocrystallized with the catalytic domain of FGF-R1 providing evidence to explain the structure-activity relationship results. This study has provided evidence to support the potential of these new tyrosine kinase inhibitors for the treatment of angiogenesis and other growth factor-related diseases including human cancers.

  DOI：

  10.1021/jm9906116

文献信息

• METHODS OF TREATMENT AND DISGNOSIS USING MODULATORS OF VIRUS-INDUCED CELLULAR GENE SEQUENCES
  申请人：Oregon Health and Science University

  公开号：EP1648997A2

  公开（公告）日：2006-04-26
• Methods of treatment and diagnosis using modulators of virus-induced cellular gene sequences
  申请人：Nelson A. Jay

  公开号：US20070087982A1

  公开（公告）日：2007-04-19

  Applicants have used microarrays, gene expression profiling, and gene silencing methods to identify and provide a plurality of ‘validated’ virus-induced cellular gene sequences (e.g., HMG20B, HRH1, NP and c-YES (src family kinases)) and pathways useful as therapeutic targets for modulation of viral-mediated cellular effects. Particular embodiments provide therapeutic compositions, and methods for modulation of viral infection, replication, maturation, progression, or other virally-related conditions or diseases, comprising inhibition of virally-induced gene sequences and gene products. Additional embodiments provide screening assays for compounds useful to modulate viral infection, replication, maturation or progression, or viral-related conditions or diseases. Further embodiments provide diagnostic and/or prognostic assays for viral infection, replication, maturation or progression. Preferably, the viruses all selected from the group consisting of retroviruses (e.g., human immunodeficiency virus (HIV), and viruses of the family Flaviviridae that includes the flaviviruses (e.g., West Nile virus (WNV), Japanese encephalitis virus (JEV), yellow fever virus (YFV) and Dengue fever virus (DEN)), and hepatitis C virus (HCV).
• ANTAGONISM OF ABCG4, LYN KINASE, AND C-CBL E3 LIGASE TO INCREASE PLATELET COUNT AS THERAPY FOR THROMBOCYTOPENIA
  申请人：WANG Nan

  公开号：US20160067301A1

  公开（公告）日：2016-03-10

  The present invention provides a method of treating a subject to increase the subject's platelet count which comprises administering to the subject an amount of one or more of an antagonist or inhibitor of ABCG4, Lyn kinase or c-CBL effective to antagonize or inhibit such ABCG4, Lyn kinase or c-CBL so as to thereby increase the subject's platelet count.
• US7211600B2
  申请人：——

  公开号：US7211600B2

  公开（公告）日：2007-05-01
• [EN] METHODS OF TREATMENT AND DISGNOSIS USING MODULATORS OF VIRUS-INDUCED CELLULAR GENE SEQUENCES<br/>[FR] METHODE DE TRAITEMENT ET DE DIAGNOSTIC A L'AIDE DE MODULATEURS DE SEQUENCES GENIQUES CELLULAIRES INDUITES PAR UN VIRUS
  申请人：UNIV OREGON HEALTH & SCIENCE

  公开号：WO2005010143A2

  公开（公告）日：2005-02-03

  Applicants have used microarrays, gene expression profiling, and gene silencing methods to identify and provide a plurality of 'validated' virus-induced cellular gene sequences (e.g., HMG20B, HRH1, NP and c-YES (src family kinases)) and pathways useful as therapeutic targets for modulation of viral-mediated cellular effects. Particular embodiments provide therapeutic compositions, and methods for modulation of viral infection, replication, maturation, progression, or other virally-related conditions or diseases, comprising inhibition of virally-induced gene sequences and gene products. Additional embodiments provide screening assays for compounds useful to modulate viral infection, replication, maturation or progression, or viral-related conditions or diseases. Further embodiments provide diagnostic and/or prognostic assays for viral infection, replication, maturation or progression. Preferably, the viruses all selected from the group consisting of retroviruses (e.g., human immunodeficiency virus (HIV), and viruses of the family Flaviviridae that includes the flaviviruses (e.g., West Nile virus (WNV), Japanese encephalitis virus (JEV), yellow fever virus (YFV) and Dengue fever virus (DEN)), and hepatitis C virus (HCV).