利索-全球专利检索

  1. Login
  2. Sign Up
Invention Grant
CN108276374B 黄酮类芳香化酶抑制剂及其制备方法与应用 失效 - 权利终止

黄酮类芳香化酶抑制剂及其制备方法与应用
Abstract:
本发明涉及一系列黄酮类芳香化酶抑制剂，通过氰甲基化反应和烷基化反应，改变了黄酮类化合物母环上的某些取代基团，合成出一系列黄酮类化合物及其衍生物。其结构通式可用权利要求书中通式表示。结构通式中，R1选自‑OH或H中的任意一种，R2选自‑H或‑OCH3或‑OH中的任意一种,R3选自‑H、‑OH或‑OCH2CN或‑OCH3中的任意一种；R4选自‑H或‑OH或‑OCH2Ph或‑2‑（2‑甲氧基‑2氧代乙基）苄氧基中的任意一种，R5选自‑H或‑OCH2Ph或‑OCH3中的任意一种，R6选自‑H或‑OH或‑OCH3中的任意一种。这些黄酮类化合物对芳香化酶有较好的抑制作用，经过活性测试，本抑制剂抑制芳香化酶的活性最高为IC50=0.251µmol/L。
Abstract(English):

The invention relates to a flavonoid aromatizing enzyme inhibitor. Through cyanomethylation reaction and alkylation reaction, some substituted groups on the mother ring of a flavonoid compound are changed and a series of flavonoid compounds and derivatives thereof are synthesized. The structural general formula can be shown in the general formula in claims. In the structural general formula, R1 isselected from any one of -OH or -H, R2 is selected from any one of -H, -OCH3 or -OH, R3 is selected from any one of -H, -OH, -OCH2CN or -OCH3, R4 is selected from any one of -H, -OH, -CH2Ph or -2-(2-methoxy-2-oxo ethyl)benzyloxy, R5 is selected from any one of -H, -OCH2Ph or -OCH3, and R6 is selected from any one of -H, -OH or -OCH3. The flavonoid compounds have good inhibition effect on aromatizing enzyme; through activity test, the maximal value IC50 of inhibiting the activity of the aromatizing enzyme by the inhibitor is equal to 0.251 [mu]mol/L.

Public/Granted literature
Patent Agency Ranking
0/0