Issue 2, 2010

Synthesis, modeling, and crystallographic study of 3,4-disubstituted-1,2,5-oxadiazoles and evaluation of their ability to decrease STAT3 activity

Abstract

STAT3 (Signal Transducer and Activator of Transcription 3) is a transcription factor constitutively activated by aberrant upstream tyrosine kinase activities in a broad spectrum of human solid and blood tumors, thus suggesting that its inhibition could represent an interesting molecular target for cancer therapy. With the aim to disclose novel scaffolds for compounds active on STAT3 the potential of the 1,2,5-oxadiazole ring was explored and several new compounds substituted at positions 3 and 4 of the heterocycle were synthesized. When tested in a dual-luciferase assay, using HCT-116 cells, some compounds showed a significant inhibition value towards STAT3. So, to give support to the biological results, modeling and crystallographic studies of representative terms of the new series were performed.

Graphical abstract: Synthesis, modeling, and crystallographic study of 3,4-disubstituted-1,2,5-oxadiazoles and evaluation of their ability to decrease STAT3 activity

Supplementary files

Article information

Article type
Concise Article
Submitted
08 Mar 2010
Accepted
08 May 2010
First published
28 May 2010

Med. Chem. Commun., 2010,1, 156-164

Synthesis, modeling, and crystallographic study of 3,4-disubstituted-1,2,5-oxadiazoles and evaluation of their ability to decrease STAT3 activity

D. Shin, D. Masciocchi, A. Gelain, S. Villa, D. Barlocco, F. Meneghetti, A. Pedretti, Y. Han, D. C. Han, B. Kwon, L. Legnani and L. Toma, Med. Chem. Commun., 2010, 1, 156 DOI: 10.1039/C0MD00057D

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