Synthesis and antiproliferative activity of some steroidal thiosemicarbazones, semicarbazones and hydrozones

• 24 steroidal hydrazone derivatives were synthesized and characterized.
• The cytotoxicity of compounds was assayed against SGC-7901 and Bel-7404 cells.
• Compound 3 and 12a–12c exhibited significant inhibitory activity to Bel-7404 cells.
• The structure–activity relationship of these compounds was discussed.

Steroidal thiosemicarbazones, semicarbazones and hydrazones have received extensive attention of scientists recently because they exhibit some biological activities such as antibacterial, antiviral and anticancer. Using different steroids as starting materials, through different chemical methods, 24 steroidal compounds with thiosemicarbazone, semicarbazone or hydrazone groups in their structures, were synthesized, characterized by IR, NMR and MS. The antiproliferative activity of the compounds was evaluated against human gastric cancer (SGC-7901) and human liver cancer (Bel-7404) cells. The structure–activity relationship of these compounds was discussed. The results showed that compound 3 and 12a–12c exhibited significant inhibitory activity to Bel-7404 cells, and IC50 values of them were 4.2, 11.0, 7.4 and 15.0 μM respectively (Cisplatin, IC50: 11.6 μM).

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