Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents.

@article{Radi2008DiscoveryAS,
  title={Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents.},
  author={Marco Radi and Emmanuele Crespan and Giorgia Botta and Federico Falchi and Giovanni Maga and Fabrizio Manetti and Valentina Corradi and Manuela Mancini and Maria Alessandra Santucci and Silvia Schenone and Maurizio Botta},
  journal={Bioorganic & medicinal chemistry letters},
  year={2008},
  volume={18 3},
  pages={1207-11}
}
A series of substituted benzoylamino-2-[(4-benzyl)thio]-1,3,4-thiadiazoles has been discovered as potent Abl tyrosine kinase inhibitors. Molecular docking simulations on the Abl tyrosine kinase were conducted in order to rationalize the SAR of the synthesized inhibitors. The most active compound identified from the enzymatic screening (6a) showed interesting inhibitory activity on Imatinib-sensitive murine myeloid 3B clone and Bcr-Abl-independent Imatinib-resistant leukemia cells. Surprisingly… CONTINUE READING

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