Synthesis, structure-activity relationships and stereochemical investigations of new tricyclic pyridazinone derivatives as potential STAT3 inhibitors = STAT3 활성 저해제 및 구조-활성 관계 규명

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Title
Synthesis, structure-activity relationships and stereochemical investigations of new tricyclic pyridazinone derivatives as potential STAT3 inhibitors = STAT3 활성 저해제 및 구조-활성 관계 규명
Author(s)
D Masciocchi; A Gelain; F Porta; F Meneghetti; A Pedretti; G Celentano; D Barlocco; L Legnani; L Toma; Byoung-Mog Kwon; A Asaid; S Villa
Bibliographic Citation
Medchemcomm, vol. 4, no. 8, pp. 1181-1188
Publication Year
2013
Abstract
Through a cell-based biological screening, the benzocinnolinone derivative (±)-2c was identified as a promising STAT3 inhibitor. Since SAR studies on a series of compounds structurally related to (±)-2c (1c, 2a-p, 3c, 4c, 6) showed that the latter had the most significant inhibitory activity, we investigated in depth its essential structural features. In particular, enantiomeric separation was performed, and the absolute configuration of the stereoisomers was assigned by theoretical and crystallographic studies. The biological evaluation highlighted that (S)-(-)-2c is twice as potent as (R)-(+)-2c.
ISSN
2040-2503
Publisher
Royal Soc Chemistry
DOI
http://dx.doi.org/10.1039/c3md00095h
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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