| 1245283-96-8

• 分子结构分类: 有机化合物 - 有机1,3-偶极化合物 - 烯丙基型1,3-偶极有机化合物
• CAS: 1245283-96-8
• 化学式: C₁₆H₁₈N₄O₁₀
• 分子量: 426.34
• InChiKey: MDLRPEGHMHIIET-UHFFFAOYSA-N

反应信息

• 作为反应物：
  描述：

  在 氯化亚砜 作用下， 以 四氢呋喃 为溶剂， 反应 0.25h， 生成
  参考文献：
  名称：

  Targeting the ICB2 site of the topoisomerase IIα promoter with a formamido-pyrrole–imidazole–pyrrole H-pin polyamide

  摘要：

  The synthesis, DNA binding characteristics and biological activity of an N-formamido pyrrole-and imidazole-containing H-pin polyamide (f-PIP H-pin, 2) designed to selectively target the ICB2 site on the topoII alpha promoter, is reported herein. Thermal denaturation, circular dichroism, isothermal titration calorimetry, surface plasmon resonance and DNase I footprinting studies demonstrated that 2 maintained the selectivity of the unlinked parent monomer f-PIP (1) and with a slight enhancement in binding affinity (K(eq) = 5 x 10(5) M(-1)) to the cognate site (5 '-TACGAT-3 '). H-pin 2 also exhibited comparable ability to inhibit NF-Y binding to 1, as demonstrated by gel shift studies. However, in stark contrast to monomer 1, the H-pin did not affect the up-regulation of topoisomerase II alpha (topoII alpha) in cells (Western blot), suggesting that the H-pin does not enter the nucleus. This study is the first to the authors' knowledge that reports such a markedly different cellular response between two compounds of almost identical binding characteristics. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2010.06.041