6-(4-Fluoro-3-nitrophenyl)imidazo[2,1-b][1,3]thiazole | 1336804-24-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 6-(4-Fluoro-3-nitrophenyl)imidazo[2,1-b][1,3]thiazole
• CAS: 1336804-24-0
• 化学式: C₁₁H₆FN₃O₂S
• 分子量: 263.252
• InChiKey: IXCJAOJASKEOMD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  91.4
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  6-(4-Fluoro-3-nitrophenyl)imidazo[2,1-b][1,3]thiazole 在 三氯氧磷 作用下， 以 乙醇 、 氯仿 为溶剂， 生成 NSC 747112
  参考文献：
  名称：

  Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors

  摘要：

  The activity of a series of imidazo[2,1-b]thiazole guanylhydrazones as inhibitors of p90 ribosomal S6 kinase 2 (RSK2) is described. It was found that a small subset of compounds show both potent inhibition of RSK2 kinase activity and tumor cell growth in vitro. Detailed study of one of the most active compounds indicates a high degree of selectivity for inhibition of RSK2 compared to a spectrum of other related kinases. Selective inhibition of the MCF-7 breast tumor cell line compared to MCF-10A non-transformed cells, as well as selective inhibition of the biomarker GSK3 provides evidence that the compounds can affect the RSK2 target in cells. (C) 2011 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2011.07.001
• 作为产物：
  描述：

  2-溴-4'-氟苯乙酮 在 硝酸 作用下， 以 丙酮 为溶剂， 反应 1.0h， 生成 6-(4-Fluoro-3-nitrophenyl)imidazo[2,1-b][1,3]thiazole
  参考文献：
  名称：

  Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors

  摘要：

  The activity of a series of imidazo[2,1-b]thiazole guanylhydrazones as inhibitors of p90 ribosomal S6 kinase 2 (RSK2) is described. It was found that a small subset of compounds show both potent inhibition of RSK2 kinase activity and tumor cell growth in vitro. Detailed study of one of the most active compounds indicates a high degree of selectivity for inhibition of RSK2 compared to a spectrum of other related kinases. Selective inhibition of the MCF-7 breast tumor cell line compared to MCF-10A non-transformed cells, as well as selective inhibition of the biomarker GSK3 provides evidence that the compounds can affect the RSK2 target in cells. (C) 2011 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2011.07.001

文献信息

• IMIDAZOOXAZOLE DERIVATIVE HAVING ANTITUMOR EFFECT, AND PHARMACEUTICAL COMPOSITION INCLUDING SAME
  申请人：Korea Institute of Science and Technology

  公开号：EP3845539A1

  公开（公告）日：2021-07-07

  Provided is a pharmaceutical composition for use in preventing and treating tumors, the pharmaceutical composition including an imidazooxazole derivative compound, a solvate, a stereoisomer, or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition is administered to an entity which has developed a tumor or is in danger of developing a tumor, and thus tumors can be prevented or treated.

  本发明提供了一种用于预防和治疗肿瘤的药物组合物，该药物组合物包括作为活性成分的咪唑恶唑衍生物化合物、其溶物、立体异构体或其药学上可接受的盐。该药物组合物用于已患肿瘤或有患肿瘤危险的实体，从而可预防或治疗肿瘤。
• Imidazooxazole derivative having antitumor effect, and pharmaceutical composition including same
  申请人：KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

  公开号：US11332479B2

  公开（公告）日：2022-05-17

  Provided is a pharmaceutical composition for preventing and treating tumors, the pharmaceutical composition including an imidazooxazole derivative compound, a solvate, a stereoisomer, or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition is administered to an entity which has developed a tumor or is in danger of developing a tumor, and thus tumors can be prevented or treated.

  本发明提供了一种用于预防和治疗肿瘤的药物组合物，该药物组合物包括作为活性成分的咪唑恶唑衍生物化合物、其溶物、立体异构体或其药学上可接受的盐。该药物组合物可用于已罹患肿瘤或有罹患肿瘤危险的实体，从而预防或治疗肿瘤。
• Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors
  作者：Aldo Andreani、Massimiliano Granaiola、Alberto Leoni、Alessandra Locatelli、Rita Morigi、Mirella Rambaldi、Lucilla Varoli、Deborah Lannigan、Jeff Smith、Dominic Scudiero、Sudhir Kondapaka、Robert H. Shoemaker

  DOI：10.1016/j.ejmech.2011.07.001

  日期：2011.9

  The activity of a series of imidazo[2,1-b]thiazole guanylhydrazones as inhibitors of p90 ribosomal S6 kinase 2 (RSK2) is described. It was found that a small subset of compounds show both potent inhibition of RSK2 kinase activity and tumor cell growth in vitro. Detailed study of one of the most active compounds indicates a high degree of selectivity for inhibition of RSK2 compared to a spectrum of other related kinases. Selective inhibition of the MCF-7 breast tumor cell line compared to MCF-10A non-transformed cells, as well as selective inhibition of the biomarker GSK3 provides evidence that the compounds can affect the RSK2 target in cells. (C) 2011 Elsevier Masson SAS. All rights reserved.