hydroximino on ring A and B displayed remarkable distinct cytotoxicities against a diversity of cancer cell types. Presence of an oxime group on ring B and a hydroxy on ring A or B resulted in a higher cytotoxicity than other structural motifs. In addition, a cholesterol-type side chain at position 17 was required for the biological activity. Our findings provide new evidence showing the relationship
化合物的侧链在其生物学功能中起着重要作用。在我们的研究中,我们发现具有不同侧链和羟基氨基在环 A 和 B 上位置的羟基亚氨基类固醇衍生物对多种癌细胞类型显示出显着不同的细胞毒性。环 B 上的肟基团和环 A 或 B 上的羟基导致比其他结构基序更高的细胞毒性。此外,生物活性需要第 17 位的胆固醇型侧链。我们的研究结果提供了新的证据,表明化学结构与生物功能之间的关系。从研究中获得的信息可能有助于设计新型化疗药物。
The present invention relates to novel chemical compounds, in particular cholest-4-en-3-one oxime derivatives and to the use thereof as medicaments, especially as cytoprotective medicaments, in particular neuroprotective, cardioprotective and/or hepatoprotective medicaments.