合成子
烷基
尿素
放射性配体
效力
组合化学
前列腺癌
IC50型
化学
谷氨酸羧肽酶Ⅱ
生物化学
立体化学
有机化学
体外
癌症
医学
内科学
作者
Narendar Reddy Gade,Jatinder Kaur,Atul Bhardwaj,Edris Ebrahimi,Jennifer Dufour,Melinda Wuest,Frank Wuest
标识
DOI:10.1021/acsmedchemlett.3c00087
摘要
We describe N-alkyl carbamoylimidazoles as readily available and highly versatile synthons for synthesizing urea-based prostate-specific membrane antigen (PSMA) inhibitors. Urea formation proceeded in high yields (>80%) at room temperature under aqueous conditions. All novel compounds were tested for their PSMA inhibitory potency in a cell-based radiometric binding assay. Compound 17 was identified as a novel high-affinity PSMA inhibitor (IC50 = 0.013 μM) suitable for developing an 18F-labeled radioligand for PET imaging of PSMA in prostate cancer.
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