Discovery of novel KRAS‒PDEδ inhibitors with potent activity in patient-derived human pancreatic tumor xenograft models

• Main Authors: Long Chen (Author), Jing Zhang (Author), Xinjing Wang (Author), Yu Li (Author), Lu Zhou (Author), Xiongxiong Lu (Author), Guoqiang Dong (Author), Chunquan Sheng (Author)
• Format: Book
• Published: Elsevier, 2022-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

KRAS‒PDEδ interaction is revealed as a promising target for suppressing the function of mutant KRAS. The bottleneck in clinical development of PDEδ inhibitors is the poor antitumor activity of known chemotypes. Here, we identified novel spiro-cyclic PDEδ inhibitors with potent antitumor activity bot...