sulfadimethoxine | 19581-29-4

• 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: sulfadimethoxine
• 英文别名: p-Amino-phenyl-6-(2,4-dimethoxypyrimidinyl)-sulfon；4-(2,6-dimethoxy-pyrimidine-4-sulfonyl)-aniline；4-(2,6-Dimethoxypyrimidin-4-yl)sulfonylaniline
• CAS: 19581-29-4
• 化学式: C₁₂H₁₃N₃O₄S
• 分子量: 295.319
• InChiKey: ZSWPSPLCCMIQIS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  113
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  sulfadimethoxine 、 甲基丙烯酰氯 在 sodium hydroxide 作用下， 以 水 、 丙酮 为溶剂， 反应 3.0h， 以1.5 g的产率得到
  参考文献：
  名称：

  Multifunctional Nanoparticles Loading with Docetaxel and GDC0941 for Reversing Multidrug Resistance Mediated by PI3K/Akt Signal Pathway

  摘要：

  The polylactic-co-glycolic acid polyethylene glycol conjugated with cell penetrating peptide R7 (PLGA PEG-R7)/ polysulfadimethoxine-folate nanoparticles loaded with docetaxel (DTX) and GDC0941 (R-7/PSD-Fol NPs) were prepared to overcome multidrug resistance (MDR) and enhance the antitumor activity. First, polysulfadimethoxine-folate was synthesized to construct the R7/PSD-Fol NPs. The R7/PSD-Fol NPs were prepared with the abilities of effective entrapment and drug loading. Due to the pH-sensitive effect of PSD-folate, the releasing of DTX and GDC0941 from the R7/PSD-Fol NPs was lower in pH 7.4 buffer solution than that in pH 5.0 buffer solution. The half maximal inhibitory concentration (IC50) of MCF-7 and resistant to doxorubicin (MCF-7/Adr) cells illustrated the cytotoxicity of R7/PSD-Fol nanoparticles by using the MTT method. The uptake of R7/PSD-Fol NPs was visualized by using the fluorescence of Rh-123 to detect the targeting effect of folate on the surface of R7/PSD-Fol NPs. The results of the cell apoptosis and the depolarization of mitochondrial membrane potential (MMP) were adopted to show the cytotoxicity of the R7/PSD-Fol NPs on MCF-7/Adr cells. The Western blot revealed the inhibition of PI3K/Akt pathway in MCF-7/Adr cells induced by R7/PSD-Fol NPs. Finally, both in vivo distribution and in vivo antitumor showed the R7/PSD-Fol NPs displayed the better distribution at tumor site and the stronger suppression of tumor growth in the tumor bearing nude mice compared with control group. It was concluded that R7/PSD-Fol NPs loaded with DTX and GDC0941 could overcome MDR and enhance the antitumor effect further.

  DOI：

  10.1021/acs.molpharmaceut.6b01045