Cui Jian-Guo, Fan Lei, Huang Li-Liang, Liu Hong-Li, Zhou Ai-Min
Department of Chemistry, Guangxi Teachers Education University, Nanning 530001, China.
Steroids. 2009 Jan;74(1):62-72. doi: 10.1016/j.steroids.2008.09.003. Epub 2008 Sep 16.
The side chain of a compound plays an important role in its biological function. In our studies, we have found that hydroximinosteroid derivatives with different side chains and position of 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 between the chemical structure and biological function. The information obtained from the studies may be useful for the design of novel chemotherapeutic drugs.
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以及A环和B环上肟基位置不同的羟肟酸甾体衍生物对多种癌细胞类型表现出显著不同的细胞毒性。B环上存在肟基且A环或B环上存在羟基会导致比其他结构基序更高的细胞毒性。此外，17位的胆固醇型侧链是生物活性所必需的。我们的发现提供了新的证据，表明化学结构与生物学功能之间的关系。从这些研究中获得的信息可能有助于新型化疗药物的设计。
