Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5445
Title: Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents
Authors: Botta, Maurizio 
Crespan, E
Botta, G
Falchi, F
Maga, G
Manetti, Fabrizio 
Corradi, V
Mancini, M
SANTUCCI M., A
Schenone, S
Botta, Maurizio 
Issue Date: 2008
Project: None 
Journal: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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-independent Imatinib-resistant leukemia cells. Surprisingly, 6a was also proved to act as differentiating inducers in human promyelocytic leukemia cells (HL-60).
Description: 
35989
URI: http://hdl.handle.net/20.500.12779/5445
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2007.11.112
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