N-(4-anilinophenyl)-2-chlorobenzamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-(4-anilinophenyl)-2-chlorobenzamide
• 化学式: C₁₉H₁₅ClN₂O
• 分子量: 322.8
• InChiKey: GMEMHQCEKIUPOP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  41.1
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• [EN] ROR GAMMA AGONISTS AS ENHANCERS OF PROTECTIVE IMMUNITY<br/>[FR] AGONISTES DE ROR GAMMA EN TANT QUE ACTIVTATEURS DE L'IMMUNITÉ PROTECTRICE
  申请人：SCRIPPS RESEARCH INST

  公开号：WO2017079120A1

  公开（公告）日：2017-05-11

  The T cell specific RORgamma isoform RORgammat has been shown to be the key lineage-defining transcription factor to initiate the differentiation program of TH17 and TC17 cells, cells that have demonstrated anti-tumor efficacy, RORgammat controls gene networks that enhance immunity including increased IL17 production and decreased immune suppression. Agonists of RORgammat have been shown to increase the basal activity of RORgammat enhancing TH17 cell proliferation. Here we show that activation of RORgammat using synthetic agonists drives proliferation of TH17 cells while decreasing levels of the immune checkpoint protein PD-1, a mechanism that should enhance anti-tumor immunity while blunting tumor associated adaptive immune resistance. Interestingly, putative endogenous agonists drive proliferation of TH17 cells but do not repress PD-1. These findings suggest that synthetic agonists of RORgammat should activate Tc17/TH17 cells, decrease the population of Tregs, repress PD-1, and produce IL17 in situ, an immune factor associated with good prognosis in cancer.

  T细胞特异性RORgamma亚型RORgammat已被证明是启动TH17和TC17细胞分化程序的关键谱系定义转录因子，这些细胞表现出抗肿瘤功效，RORgammat控制增强免疫的基因网络，包括增加IL17产生和减少免疫抑制。已经证明RORgammat的激动剂可以增加RORgammat的基础活性，增强TH17细胞增殖。在这里，我们展示了使用合成激动剂激活RORgammat会驱动TH17细胞增殖，同时降低免疫检查点蛋白PD-1的水平，这一机制应该增强抗肿瘤免疫，同时减弱肿瘤相关的适应性免疫抵抗。有趣的是，推测的内源性激动剂会驱动TH17细胞增殖，但不会抑制PD-1。这些发现表明，RORgammat的合成激动剂应该能够激活Tc17/TH17细胞，减少Tregs的数量，抑制PD-1，并在原位产生IL17，这是与癌症良好预后相关的免疫因子。
• ANTI-VIRAL TREATMENT AND ASSAY TO SCREENFOR ANTI-VIRAL AGENT
  申请人：Severson Bill

  公开号：US20130085133A1

  公开（公告）日：2013-04-04

  The present disclosure relates to novel compounds of formulas (1) through (19) and to a method for treating humans infected with a virus including various respiratory viruses such as members of the Paramyxoviridae family (respiratory syncytial virus (RSV), human metapneumovirus (HMPV), human parainfluenza virus (HPIV), measles virus, and mumps virus) with a compound of formulas (1) through (19). The present disclosure also relates to a cytopathic effect (CPE)-based assay that will assess virus-induced CPE for screening of compounds for treating viral diseases or inhibiting a virus.