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

…, E Crespan, G Botta, F Falchi, G Maga, F Manetti…

Index: Radi, Marco; Crespan, Emmanuele; Botta, Giorgia; Falchi, Federico; Maga, Giovanni; Manetti, Fabrizio; Corradi, Valentina; Mancini, Manuela; Santucci, Maria Alessandra; Schenone, Silvia; Botta, Maurizio Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 3 p. 1207 - 1211

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Citation Number: 42

Abstract

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- ...

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