3-[8-(aminomethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-methyl-3-indolyl)-1H-pyrrole-2,5-dione | 151342-35-7

• 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: 3-[8-(aminomethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-methyl-3-indolyl)-1H-pyrrole-2,5-dione
• 英文别名: Ro 31-8425；3-[8-(Aminomethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-methylindol-3-yl)pyrrole-2,5-dione
• CAS: 151342-35-7
• 化学式: C₂₆H₂₄N₄O₂
• mdl: MFCD00906977
• 分子量: 424.502
• InChiKey: QQKKPWJFHBFCTH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  32
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  82
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  8-(acetoxymethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indole 在 2,4,6-三甲基吡啶 、 ammonium hydroxide 、 三乙胺 作用下， 以 乙醚 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 93.5h， 生成 3-[8-(aminomethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-methyl-3-indolyl)-1H-pyrrole-2,5-dione
  参考文献：
  名称：

  Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction

  摘要：

  The protein kinase inhibitor staurosporine has been used to design a series of selective bisindolylmaleimide inhibitors of protein kinase C (PKC). Guided by molecular graphics, conformational restriction of the cationic side chain has led to ATP competitive inhibitors of improved potency and selectivity. Two compounds have been further evaluated and were shown to inhibit PKC of human origin and prevent T-cell activation in a human allogeneic mixed lymphocyte reaction. One of these compounds was orally absorbed in mice and antagonized a phorbol ester induced paw edema in a dose-dependent manner. This compound also selectively inhibited the secondary T-cell mediated response in a developing adjuvant arthritis model in rats and provides evidence for the potential use of PKC inhibitors as therapeutic immunomodulators.

  DOI：

  10.1021/jm00053a003

文献信息

• [EN] METHODS FOR HAIR FOLLICLE STEM CELL PROLIFERATION<br/>[FR] PROCÉDÉS POUR LA PROLIFÉRATION DES CELLULES SOUCHES DES FOLLICULES PILEUX
  申请人：FREQUENCY THERAPEUTICS INC

  公开号：WO2018191350A1

  公开（公告）日：2018-10-18

  The present invention relates to compositions of Sonic Hedgehog (Shh) pathway activators and Wnt agonists and methods of using them to induce self-renewal of hair follicle stem cells, including inducing the hair follicle stem cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair follicle epithelial cells.

  本发明涉及Sonic Hedgehog（Shh）通路激活剂和Wnt激动剂的组合物，以及使用它们诱导毛囊干细胞自我更新的方法，包括诱导毛囊干细胞增殖，同时保持子细胞具有分化为毛囊上皮细胞的能力。
• METHODS FOR HAIR FOLLICLE STEM CELL PROLIFERATION
  申请人：Frequency Therapeutics, Inc.

  公开号：US20200121681A1

  公开（公告）日：2020-04-23

  The present invention relates to compositions of minoxidil and Sonic Hedgehog (Shh) pathway activators and optionally, Wnt agonists and methods of using them to induce self-renewal of hair follicle stem cells, including inducing the hair follicle stem cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair follicle epithelial cells.

  本发明涉及米诺地尔和Sonic Hedgehog (Shh)途径激活剂以及可选的Wnt激动剂的组合物，以及使用它们诱导毛囊干细胞的自我更新的方法，包括诱导毛囊干细胞增殖，同时保持子细胞具有分化为毛囊上皮细胞的能力。
• MULTIPLEXED KINASE INHIBITOR BEADS AND USES THEREOF
  申请人：University of North Carolina at Chapel Hill

  公开号：US20140243239A1

  公开（公告）日：2014-08-28

  This invention is directed to a multi-analyte column comprising two or more layers with a first solid support having specific binding affinity for kinases and a second solid support having non-specific binding affinity for kinases. Methods are also provided, including methods of detecting low abundance kinases, predicting resistance to chemotherapy, determining cancer prognosis, and improving the effectiveness of a treatment regimen.

  本发明涉及一种多分析物柱，包括两个或更多层，第一固体支持体具有对激酶具有特异性结合亲和力，第二固体支持体具有对激酶具有非特异性结合亲和力。还提供了方法，包括检测低丰度激酶的方法，预测对化疗的耐药性，确定癌症预后以及提高治疗方案的有效性。
• Substituierte Pyrrole
  申请人：F. HOFFMANN-LA ROCHE AG

  公开号：EP0384349A1

  公开（公告）日：1990-08-29

  Die Pyrrolderivate der Formel worin R¹ bis R⁸, R, X, Y und m die in der Beschreibung angegebene Bedeutung haben, sind therapeutisch aktive Sub­stanzen, insbesondere zur Verwendung als antiinflamma­torisch, immunologisch, onkologisch, bronchopulmonär und kardiovaskulär aktive Substanzen oder als Wirkstoffe in der Behandlung von Asthma oder AIDS. Sie werden hergestellt aus entsprechenden Furandion­derivaten, worin O für =N-R, X und Y steht.

  式中的吡咯衍生物 其中 R¹ 至 R⁸、R、X、Y 和 m 具有说明中给出的含义，是具有治疗活性的物质，特别是可用作抗炎、免疫、肿瘤、支气管和心血管活性物质或治疗哮喘或艾滋病的活性物质。 它们由相应的呋喃二酮衍生物制得，其中 O 代表 =N-R、X 和 Y。
• Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using GSK3 inhibitors: III
  申请人：Frequency Therapeutics, Inc.

  公开号：US10016507B2

  公开（公告）日：2018-07-10

  The present invention relates to compositions and methods of inducing the self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair cells.

  本发明涉及诱导干/祖支持细胞自我更新的组合物和方法，包括诱导干/祖细胞增殖，同时保持子细胞分化成毛细胞的能力。