Discovery of novel Bcr-AblT315I inhibitors with flexible linker. Part 1: Confirmation optimization of phenyl-1H-indazol-3-amine as hinge binding moiety.

@article{Pan2019DiscoveryON,
  title={Discovery of novel Bcr-AblT315I inhibitors with flexible linker. Part 1: Confirmation optimization of phenyl-1H-indazol-3-amine as hinge binding moiety.},
  author={X. Pan and Liyuan Liang and Y. Sun and Ru Si and Qingqing Zhang and J. Wang and Jia Fu and J. Zhang},
  journal={European journal of medicinal chemistry},
  year={2019},
  volume={178},
  pages={
          232-242
        }
}
As a continuation to our research, a series of novel Bcr-Abl inhibitors incorporated with 6-phenyl-1H-indazol-3-amine as hinge binding moiety (HBM) were developed based on confirmation analysis. Biological results indicated that these compounds exhibited an enhanced inhibition against Bcr-AblWT and Bcr-AblT315I in kinases assays, along with improved anti-proliferative activities in K562 cell assays. In particular, compound Y9 displayed comparable potency with that of imatinib. It potently… Expand

References

SHOWING 1-10 OF 25 REFERENCES
Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1H-indazol-3-amine.
  • 8
Discovery of novel Bcr-Abl inhibitors with diacylated piperazine as the flexible linker.
  • 10
  • PDF
Synthesis and biological evaluation of novel aromatic-heterocyclic biphenyls as potent anti-leukemia agents.
  • 6
Nilotinib: a novel, selective tyrosine kinase inhibitor.
  • 75
Design, synthesis and biological activities of Nilotinib derivates as antitumor agents.
  • 14
...
1
2
3
...