3-<1-methyl-4-<1-methyl-4-<2'-(2-aminoethyl)-2,4'-bithiazole-4-carboxamido>pyrrole-2-carboxamido>pyrrole-2-carboxamido>propionamidine bis(trifluoroacetate) | 144332-52-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-<1-methyl-4-<1-methyl-4-<2'-(2-aminoethyl)-2,4'-bithiazole-4-carboxamido>pyrrole-2-carboxamido>pyrrole-2-carboxamido>propionamidine bis(trifluoroacetate)
• CAS: 144332-52-5
• 化学式: 2C₂HF₃O₂*C₂₄H₂₈N₁₀O₃S₂
• 分子量: 796.731
• InChiKey: APXYZIBIEKBCRC-UHFFFAOYSA-N

反应信息

• 作为产物：
  描述：

  3-<1-methyl-4-<1-methyl-4-<2'-<2-(N-tert-butoxycarbonyl)aminoethyl>-2,4'-bithiazole-4-carboxamido>pyrrole-2-carboxamido>pyrrole-2-carboxamido>propionamidine hydrochloride 、 三氟乙酸 以 N,N-二甲基甲酰胺 为溶剂， 反应 0.67h， 以55%的产率得到3-<1-methyl-4-<1-methyl-4-<2'-(2-aminoethyl)-2,4'-bithiazole-4-carboxamido>pyrrole-2-carboxamido>pyrrole-2-carboxamido>propionamidine bis(trifluoroacetate)
  参考文献：
  名称：

  Synthesis, determination of sequence selective DNA minor groove binding and biological evaluation of hybrid bithiazole-linked netropsin derivatives

  摘要：

  A series of hybrid molecules have been synthesized which result from the combination of a DNA sequence-specific ligand (netropsin) coupled to a DNA-interactive structural component of bleomycins (bithiazole). The DNA binding affinities as well as the cytostatic activity and their in vitro activity against a wide variety of viruses have been determined. Most of the new agents retain the DNA binding capacity of netropsin and distamycin, and force field and Pi calculations reveal the important role of the arc of curvature of these compounds in their binding to DNA. Like netropsin, the evaluated molecules did not show significant antiviral activity, but one of them demonstrated enhanced cytostatic activity against both human and murine tumor cell lines.

  DOI：

  10.1016/0223-5234(92)90146-r