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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

Authors 

D MasciocchiA GelainF PortaF MeneghettiA PedrettiG CelentanoD BarloccoL LegnaniL TomaByoung-Mog KwonA AsaidS Villa

Publisher 

Royal Society of Chemistry

Issue Date 

2013

Citation 

MedChemComm, vol. 4, no. 8, pp. 1181-1188

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

Link 

http://dx.doi.org/10.1039/c3md00095h

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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