谷氨酸羧肽酶Ⅱ
取代基
化学
配体(生物化学)
连接器
吡啶
立体化学
戒指(化学)
组合化学
生物化学
前列腺
医学
受体
药物化学
癌症
内科学
有机化学
操作系统
计算机科学
作者
Ryo Nakajima,Zora Nováková,W. Tueckmantel,L. Motlova,Cyril Bařinka,Alan P. Kozikowski
标识
DOI:10.1021/acsmedchemlett.8b00318
摘要
The design and synthesis of prostate specific membrane antigen (PSMA) ligands derived from 2-aminoadipic acid, a building block that has not previously been used to construct PSMA ligands, are reported. The effects of both the linker length and of an N-substituent of our PSMA ligands were probed, and X-ray structures of five of these ligands bound to PSMA were obtained. Among the ligands disclosed herein, 13b showed the highest inhibitory activity for PSMA. As ligand 13b can readily be radiolabeled since its fluorine atom is adjacent to the nitrogen atom of its pyridine ring, the use of this and related compounds as theranostics can be pursued.
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