Chemistry Department, Faculty of Science, Taibah University, Yanbu 46423, Saudi Arabia.
Chemistry Department, Faculty of Science, Alexandria University, P.O. 426 Ibrahemia, Alexandria 21321, Egypt.
Biomolecules. 2024 Jul 8;14(7):811. doi: 10.3390/biom14070811.
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.
一类新型的吡唑基亚甲基-2-硫代-咪唑烷-4-酮衍生物被合理设计和合成，旨在探索它们作为前列腺癌治疗药物的潜力。合成的化合物针对 ARLNCaP、ARPC-3 和 Wi38 细胞系进行了抗癌活性的生物分析。在孵育 24 小时后，观察到对 ARLNCaP 的 IC 值范围在 10.27 ± 0.14 和 109.72 ± 2.06 µM 之间。在存在 1 nM DHT 的情况下，化合物 、和 孵育 48 小时后，IC 值为 05.22 ± 0.12 至 11.75 ± 0.07 µM，对 ARLNCaP 具有更高的选择性。此外，化合物 和 显著诱导 Caspase 3 积累，减少细胞周期各阶段的 DNA 含量，并最终导致 ARLNCaP 细胞生长停滞，这一点通过细胞凋亡分析得到了证实。这些发现表明，这些雄激素受体阻滞剂类似物具有作为有效的前列腺癌治疗药物进一步研究的潜力。
