Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
Lomonosov Moscow State University, Chemistry Dept., Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
Bioorg Med Chem Lett. 2022 Sep 1;71:128840. doi: 10.1016/j.bmcl.2022.128840. Epub 2022 May 31.
We report an improved series of ligands targeting prostate specific membrane antigen (PSMA). The new compounds were designed by the introduction of changes in the structure of the aromatic fragment at ε-nitrogen atom of lysine that resulted in improved biological parameters. Some of them demonstrated high selectivity and nanomolar IC values. We synthesized and tested two conjugates with a fluorescent label Sulfo-Cy5 as an example of the use of the obtained PSMA inhibitors as a basis for the creation of diagnostic preparations.
我们报告了一系列针对前列腺特异性膜抗原（PSMA）的改良配体。新化合物的设计是通过改变赖氨酸ε-氮原子上芳环片段的结构来实现的，这导致了生物参数的改善。其中一些化合物表现出高选择性和纳摩尔 IC 值。我们合成并测试了两种带有荧光标记 Sulfo-Cy5 的缀合物，以此为例，使用所获得的 PSMA 抑制剂作为创建诊断制剂的基础。
