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

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Title
Synthesis, modeling, and crystallographic study of 3,4-disubstituted-1,2,5-oxadiazoles and evaluation of their ability to decrease STAT3 activity
Author(s)
Shin Dae Seop; D Masciocchi; A Gelain; S Villa; D Barlocco; F Meneghetti; A Pedretti; han young min; Dong Cho Han; Byoung-Mog Kwon; L Legnani; L Toma
Bibliographic Citation
Medchemcomm, vol. 1, no. 2, pp. 156-164
Publication Year
2010
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.
ISSN
2040-2503
Publisher
Royal Soc Chemistry
DOI
http://dx.doi.org/10.1039/c0md00057d
Type
Article
Appears in Collections:
Division of Biomedical Research > Personalized Genomic Medicine Research Center > 1. Journal Articles
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