Thiohydrazides in the Synthesis of Functionalized Extranuclear Heterosteroids

The study investigates the synthesis of functionalized heterocyclic steroid derivatives using oxamic acid thiohydrazides, which show promise in drug discovery due to their biological activity. The research successfully creates various steroidal derivatives, such as 1,3,4-thiadiazoles, pyrazolines, pyridazines, and thiadiazines, which exhibit significant antiproliferative activity against breast and prostate cancer cell lines. Notably, some compounds demonstrate higher cytotoxicity than cisplatin, a standard chemotherapy drug, and 17-[1′,3′,4′]thiadiazine-substituted androstenes show significant effects against androgen receptor-positive prostate cancer cells, surpassing bicalutamide. These findings suggest the potential of these derivatives as selective anticancer agents, particularly for hormone-receptor-positive cancers, by modulating pathways like AR, ERK 1/2, NF-κB, and PARP.