Synthesis and antiproliferative activity of D-ring substituted steroidal benzamidothiazoles

• A series of novel D-ring substituted steroidal benzamidothiazoles were designed and synthesized.
• Antiproliferative activities of the newly synthesized derivatives were evaluated against two human cancer cell lines.
• Compounds 8b, 8d and 8g exhibited moderate antiproliferative activities against SKOV-3 cells.

Using progesterone as the starting material, we synthesized a series of steroidal derivatives possessing a D-ring substituted benzamidothiazole. All of the final structures were reported and identified by NMR and HRMS spectrometry for the first time. The antiproliferative activity of the synthesized compounds against PC-3 (human prostate cancer cell line) and SKOV-3 (ovarian cancer cells) were investigated. The preliminary results showed that compounds 8b, 8d and 8g possessed moderate antiproliferative activities.

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