NLCQ-1 | 221292-08-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: NLCQ-1
• 英文别名: 4-[3-(2-nitro-1-imidazolyl)-propylamino]-7-chloroquinoline hydrochloride；4-(3-(2-Nitro-1-imidazolyl)-propylamino)-7-chloroquinoline hydrochloride；7-chloro-N-[3-(2-nitroimidazol-1-yl)propyl]quinolin-4-amine;hydrochloride
• CAS: 221292-08-6
• 化学式: C₁₅H₁₄ClN₅O₂*ClH
• 分子量: 368.222
• InChiKey: LWTUZIMLIKOKDI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.92
• 重原子数：
  24
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  88.6
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  4-[3-(2-nitro-1-imidazolyl)-propylamino]-7-chloroquinoline 在 盐酸 作用下， 以 乙醚 、 丙酮 为溶剂， 以100%的产率得到NLCQ-1
  参考文献：
  名称：

  Method of Treating Latent Tuberculosis

  摘要：

  本发明揭示了2-硝基咪唑基-烷基氨基喹啉及其含量，对于治疗结核病有用。本发明还揭示了使用2-硝基咪唑基-烷基氨基喹啉及其含量治疗结核病的方法。

  公开号：

  US20080076797A1

文献信息

• Induction of tumor hypoxia for cancer therapy
  申请人：Virginia Commonwealth University

  公开号：US10159676B2

  公开（公告）日：2018-12-25

  Methods and compositions for enhancing the ability of hypoxia-activated bioreductive agents to kill tumor cells within solid tumors are provided. Local regions of hypoxia are created within a tumor, or within a region containing a tumor, resulting in enhanced activation of hypoxia-activated bioreductive agents (e.g. tirapazamine) within the local region. The activated hypoxia-activated bioreductive agents kill tumor cells in the hypoxic region by catalyzing DNA stand breakage within the tumor cells. Because the activity is localized, side effects that typically occur as a result of systemic administration of bioreductive agents are reduced.

  本文提供了增强缺氧激活生物还原剂杀死实体瘤内肿瘤细胞能力的方法和组合物。在肿瘤内或含有肿瘤的区域内形成局部缺氧区域，从而增强局部区域内缺氧激活的生物还原剂（如替拉帕扎胺）的活化。活化的缺氧活化生物还原剂通过催化肿瘤细胞内的 DNA 支架断裂，杀死缺氧区域内的肿瘤细胞。由于生物还原剂的活性是局部的，因此可减少因全身使用生物还原剂而产生的副作用。
• Compositions and methods for immune-mediated cancer therapy
  申请人：Teclison Limited

  公开号：US11534445B2

  公开（公告）日：2022-12-27

  Disclosed herein are methods and compositions for enhancing an immune response to a solid tumor in a subject. In some embodiments, a method comprises: (a) administering to the subject a hypoxia-activated bioreductive agent (HABA); (b) inducing hypoxia by (i) administering a hypoxia-inducing agent to the subject or (ii) embolizing one or more blood vessels supplying the solid tumor; and (c) administering an immune checkpoint inhibitor prior to, simultaneously with, or subsequent to step (b) in an amount effective to enhance an immune response to the solid tumor, as compared to an immune response in the absence of the immune checkpoint inhibitor. Kits for use in the disclosed methods are also provided.

  本文公开了用于增强受试者对实体瘤的免疫应答的方法和组合物。在一些实施方案中，方法包括(a) 向受试者施用缺氧激活的生物还原剂（HABA）；(b) 通过(i)向受试者施用缺氧诱导剂或(ii)栓塞供应实体瘤的一个或多个血管来诱导缺氧；以及(c)在步骤(b)之前、同时或之后施用免疫检查点抑制剂，施用量有效于增强对实体瘤的免疫应答，与不施用免疫检查点抑制剂时的免疫应答相比。还提供了用于所公开方法的试剂盒。
• Novel 3-Nitro-1<i>H</i>-1,2,4-triazole-Based Aliphatic and Aromatic Amines as Anti-Chagasic Agents
  作者：Maria V. Papadopoulou、Bernadette Bourdin Trunz、William D. Bloomer、Caroline McKenzie、Shane R. Wilkinson、Chaiya Prasittichai、Reto Brun、Marcel Kaiser、Els Torreele

  DOI：10.1021/jm201215n

  日期：2011.12.8

  A series of novel 2-nitro-1H-imidazole- and 3-nitro-1H-1,2,4-triazole-based aromatic and aliphatic amines were screened for antitrypanosomal activity and mammalian cytotoxicity by the Drugs for Neglected Diseases initiative (DNDi). Out of 42 compounds tested, 18 3-nitro-1,2,4-triazoles and one 2-nitroimidazole displayed significant growth inhibitory properties against T. cruzi amastigotes (IC50 ranging from 40 nM to 1.97 mu M), without concomitant toxicity toward the host cells (L6 cells), having selectivity indices (SI) 44-1320. Most (16) of these active compounds were up to 33.8-fold more potent than the reference drug benznidazole, tested in parallel. Five novel 3-nitro-1,2,4-triazoles were active against bloodstream-form (BSF) T. b. rhodesiense trypomastigotes (IC50 at nM levels and SI 220-993). An NADH-dependent nitroreductase (TbNTR) plays a role in the antiparasitic activity because BSF T. b. brucei trypomastigotes with elevated TbNTR levels were hypersensitive to tested compounds. Therefore, a novel class of affordable 3-nitro-1,2,4-triazole-based compounds with antitrypanosomal activity has been identified.
• TREATMENT OF CANCER USING HYPOXIA ACTIVATED PRODRUGS
  申请人：Threshold Pharmaceuticals, Inc.

  公开号：EP2350664A1

  公开（公告）日：2011-08-03
• TREATMENT OF CANCER USING THE HYPOXIA ACTIVATED PRODRUG TH-302 IN COMBINATION WITH DOCETAXEL OR PEMETREXED
  申请人：ImmunoGenesis, Inc.

  公开号：EP2350664B1

  公开（公告）日：2021-05-19