| 1017571-59-3

• 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
• CAS: 1017571-59-3
• 化学式: C₂₅H₃₅F₃N₄O₂Si
• 分子量: 508.659
• InChiKey: ZYSJIWSCAIUTSH-JXFKEZNVSA-N

反应信息

• 作为反应物：
  描述：

  在 四丁基氟化铵 作用下， 以 四氢呋喃 为溶剂， 反应 0.67h， 以88%的产率得到(9S,12S)-12-(hydroxymethyl)-8-methyl-9-propan-2-yl-3-(trifluoromethyl)-1,2,8,11-tetrazatetracyclo[12.2.1.04,16.07,15]heptadeca-2,4(16),5,7(15),14(17)-pentaen-10-one
  参考文献：
  名称：

  Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/π interaction

  摘要：

  Phorbol ester-type tumor promoters such as indolactarn-V (IL-V, 1) bind to the Cl domains of protein kinase C (PKC) isozymes. A more convenient method to investigate the interaction between each tumor promoter and PKC C1 domain is needed. Focusing on our recent finding that the indole ring of IL-V is involved in the CH/pi interaction with Pro-11 of the PKC delta-CIB domain, we developed new fluorescent probes (2-4) from IL-V by forming a pyrroloindazole ring. Compound 2 without a substituent at the pyrroloindazole ring bound most strongly to PKC C1 domains with a potency similar to IL-V, but its fluorescent intensity was the weakest of any of the probes, Although the binding affinity of 3 with a methyl group was significantly weaker than that of IL-V, 4 with a trifluoromethyl group showed moderate affinity and the most potent fluorescence intensity. The fluorescence intensity and emission maxima of 4 changed significantly when bound to the PKC delta-CIB peptide in both the presence and absence of phosphatidylserine. These results suggest that 4 could be a useful probe for analyzing the interaction of tumor promoters with PKC C1 domains. (c) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2007.10.045
• 作为产物：
  描述：

  在 4-二甲氨基吡啶 、 三乙胺 、 对甲苯磺酰氯 作用下， 以 乙醚 为溶剂， 以48%的产率得到
  参考文献：
  名称：

  Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/π interaction

  摘要：

  Phorbol ester-type tumor promoters such as indolactarn-V (IL-V, 1) bind to the Cl domains of protein kinase C (PKC) isozymes. A more convenient method to investigate the interaction between each tumor promoter and PKC C1 domain is needed. Focusing on our recent finding that the indole ring of IL-V is involved in the CH/pi interaction with Pro-11 of the PKC delta-CIB domain, we developed new fluorescent probes (2-4) from IL-V by forming a pyrroloindazole ring. Compound 2 without a substituent at the pyrroloindazole ring bound most strongly to PKC C1 domains with a potency similar to IL-V, but its fluorescent intensity was the weakest of any of the probes, Although the binding affinity of 3 with a methyl group was significantly weaker than that of IL-V, 4 with a trifluoromethyl group showed moderate affinity and the most potent fluorescence intensity. The fluorescence intensity and emission maxima of 4 changed significantly when bound to the PKC delta-CIB peptide in both the presence and absence of phosphatidylserine. These results suggest that 4 could be a useful probe for analyzing the interaction of tumor promoters with PKC C1 domains. (c) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2007.10.045