Wei Zheng, Yong Huang, Yi Xie, Tingyu Yang, Xuebo Cheng, Hualong Chen, Chengze Li, Zeng Jiang, Ziyue Yu, Zhongjing Li, Lu Zhang, Leilei Yuan, Yajing Liu, Ying Liang, Zehui Wu
Compounds 8a - j were designed to adjust the mode of interaction and lipophilicity of FTT by scaffold hopping and changing the length of the alkoxy groups. Compounds 8a , 8d , 8g , and BIBD-300 were screened for high-affinity PARP-1 through enzyme inhibition assays and are worthy of further evaluation. PET imaging of MCF-7 subcutaneous tumors with moderate expression of PARP-1 showed that compared to [18 F]FTT, [ 18 F]8a , [ 18 F]8d , and [ 18 F]8g exhibited greater nonspecific uptake, a lower target-to-nontarget ratio, and severe defluorination, while [18 F]BIBD-300 exhibited lower nonspecific uptake and a greater target-to-nontarget ratio...
April 12, 2024: Molecular Pharmaceutics