7α-(4'-dansylamino)phenylthio-4-androstene-3,17-dione | 127716-71-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 7α-(4'-dansylamino)phenylthio-4-androstene-3,17-dione
• CAS: 127716-71-6
• 化学式: C₃₇H₄₂N₂O₄S₂
• 分子量: 642.883
• InChiKey: BQNTUGPRWVRAJU-AHGGWJOESA-N

反应信息

• 作为产物：
  描述：

  丹酰氯 、 7α-<(4-aminophenyl)thio>androst-4-ene-3,17-dione 在 sodium carbonate 作用下， 以 丙酮 为溶剂， 反应 10.0h， 以14.3%的产率得到7α-(4'-dansylamino)phenylthio-4-androstene-3,17-dione
  参考文献：
  名称：

  Synthesis and biochemistry of fluorescent aromatase inhibitors

  摘要：

  Effective aromatase inhibitors have been developed that contain aryl functionalities at the 7 alpha-position of the steroid nucleus. The exact interactions of 7 alpha-substituted androstenediones with the active site of aromatase is unknown. Fluorescent derivatives may provide a useful spectroscopic method for examining the binding of these inhibitors to the microsomal complex and purified aromatase protein. Dinitrophenyl, dansyl, and naphthyl derivatives of 7 alpha-(4'-amino)phenylthio-4-androstene-3,17-dione and androstenedione were synthesized as potential fluorescent agents. An in vitro assay with human placental microsomes was used to evaluate aromatase inhibitory properties. These fluorescent compounds were effective competitive inhibitors and have apparent Ki values ranging from 24.1 to 86.7 nM.

  DOI：

  10.1016/0039-128x(90)90008-y