Design and synthesis of benzodiazepines as brain penetrating PARP-1 inhibitors

• Main Authors: Jiang Yu (Author), Wenfeng Gou (Author), Haihua Shang (Author), Yating Cui (Author), Xiao Sun (Author), Lingling Luo (Author), Wenbin Hou (Author), Tiemin Sun (Author), Yiliang Li (Author)
• Format: Book
• Published: Taylor & Francis Group, 2022-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

The poly (ADP-ribose) polymerase (PARP) inhibitors play a crucial role in cancer therapy. However, most approved PARP inhibitors cannot cross the blood-brain barrier, thus limiting their application in the central nervous system. Here, 55 benzodiazepines were designed and synthesised to screen brain...