Study on the Synthesis and Bioactivity of Diosgenin Antitumor Derivatives

Synthesis and Antitumor Activity of Diosgenin Hydroxamic Acid and Quaternary Phosphonium Salt Derivatives

“…15−20 In our previous studies, three series of nitrogen-containing derivatives were reported for antitumor activity. 21,22 So it was obvious that the antitumor activity of the A ring derivatives is generally better than that of the F ring derivatives. Nitrogen-containing heterocycles and quaternary ammonium salt derivatives have good activity, and it may be that nitrogen-containing heterocycles have unique biological activity and low biotoxicity, which play an important role in the structural modification of drug molecules.…”

“…In our previous studies, we tested the enzyme activity of derivatives with better inhibitory activity and lower biotoxicity. 21 The EGFR enzyme was used to investigate the survival rate of cells at different concentrations, and the corresponding IC 50 value was calculated to further verify the good activity of the derivatives. Therefore, the enzyme activity test was not repeated.…”

“…Based on the above properties of diosgenin, several research groups modified the C-3 hydroxyl group of the diosgenin A ring and C-26 of the diosgenin F ring. − In our previous studies, three series of nitrogen-containing derivatives were reported for antitumor activity. , So it was obvious that the antitumor activity of the A ring derivatives is generally better than that of the F ring derivatives. Nitrogen-containing heterocycles and quaternary ammonium salt derivatives have good activity, and it may be that nitrogen-containing heterocycles have unique biological activity and low biotoxicity, which play an important role in the structural modification of drug molecules. − Meta derivatives appropriately introduce hydrophilic groups to increase their water solubility, so as to obtain better pharmacological activities …”

“…Gifitinib is an epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) and the first NSCLC targeted drug with the most mature research. In our previous studies, we tested the enzyme activity of derivatives with better inhibitory activity and lower biotoxicity . The EGFR enzyme was used to investigate the survival rate of cells at different concentrations, and the corresponding IC 50 value was calculated to further verify the good activity of the derivatives.…”