Design, Synthesis, Characterization, and Cytotoxicity of New Pyrazolylmethylene-2-thioxoimidazolidin-4-one Derivatives towards Androgen-Sensitive LNCaP Prostate Cancer Cells.

A new class of pyrazolylmethylene-2-thioxoimidazolidin-4-one derivatives were rationally designed and synthesized with the aim of exploring their potential as treatments for prostate cancer. The synthesized compounds were biologically analyzed for their anticancer effects against ARLNCaP, ARPC-3, and Wi38 cell lines. The observed IC values against ARLNCaP ranged between 10.27 ± 0.14 and 109.72 ± 2.06 µM after 24 h of incubation. Compounds , , and recorded IC values of 05.22 ± 0.12 to 11.75 ± 0.07 µM after 48 h incubation in the presence of 1 nM DHT, with higher selectivity towards ARLNCaP. Moreover, compounds and significantly induced Caspase 3 accumulation, reduced DNA content at the various stages of the cell cycle, and ultimately caused ARLNCaP cell growth arrest, as confirmed by cell apoptosis assays. These findings suggest that these analogues of androgen receptor blockers have promising potential for further investigation as effective treatments for prostate cancer.