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Synthesis And Evaluation Of Some Steroidal Oximes As Cytotoxic Agents: Structure/Activity Studies (Ii), Jianguo Cui, Lei Fan, Yanmin Huang, Yi Xin, Aimin Zhou
Synthesis And Evaluation Of Some Steroidal Oximes As Cytotoxic Agents: Structure/Activity Studies (Ii), Jianguo Cui, Lei Fan, Yanmin Huang, Yi Xin, Aimin Zhou
Chemistry Faculty Publications
Hydroximinosteroids isolated from marine sponges display a variety of biological functions including cytotoxicity and anti-virus. In this study, we synthesized a series of hydroximinosteroid derivatives with a different functional group on the ring A or B and various side chains at position 17, and analyzed the cytotoxicity of these compounds against sk-Hep-1, H-292, PC-3 and Hey-1B cancer cells. Our results revealed that although a cholesterol-type side chain at position 17 is required for the biological activity of the compounds as we previously confirmed, elimination of the 4,5-double bond augmented the cytotoxic activity for the steroidal oximes. In addition, the presence …
Synthesis And Evaluation Of Some Steroidal Oximes As Cytotoxic Agents: Structure/Activity Studies (I), Jianguo Cui, Lei Fan, Li Liang Huang, Hong Li Liu, Aimin Zhou
Synthesis And Evaluation Of Some Steroidal Oximes As Cytotoxic Agents: Structure/Activity Studies (I), Jianguo Cui, Lei Fan, Li Liang Huang, Hong Li Liu, Aimin Zhou
Chemistry Faculty Publications
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 …