Chemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russia.
Laboratory of Biomedical Nanomaterials, National University of Science and Technology MISIS, 4 Leninskiy pr, Moscow 119049, Russia.
Int J Mol Sci. 2023 Jul 11;24(14):11327. doi: 10.3390/ijms241411327.
Prostate cancer is the second most common cancer among men. We designed and synthesized new ligands targeting prostate-specific membrane antigen and suitable for bimodal conjugates with diagnostic and therapeutic agents. studies of the affinity of the synthesized compounds to the protein target have been carried out. Based on these ligands, a series of bimodal conjugates with a combination of different mitosis inhibitors and antiandrogenic drugs were synthesized. The cytotoxicity of the compounds obtained was investigated on three different cell lines. The efficacy of the two obtained conjugates was evaluated in xenograft models of prostate cancer. These compounds have been shown to be highly effective in inhibiting the growth of PSMA-expressing tumors.
前列腺癌是男性中第二常见的癌症。我们设计并合成了针对前列腺特异性膜抗原的新型配体，这些配体适合与诊断和治疗剂结合形成双模态共轭物。已经对合成化合物与蛋白质靶标的亲和力进行了研究。基于这些配体，合成了一系列具有不同有丝分裂抑制剂和抗雄激素药物组合的双模态共轭物。对获得的化合物在三种不同细胞系上的细胞毒性进行了研究。在前列腺癌的异种移植模型中评估了两种获得的共轭物的疗效。这些化合物在抑制 PSMA 表达肿瘤的生长方面表现出了很高的疗效。
