Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors

[Image: see text] We optimized our previously reported proline-based STAT3 inhibitors into an exciting new series of (R)-azetidine-2-carboxamide analogues that have sub-micromolar potencies. 5a, 5o, and 8i have STAT3-inhibitory potencies (IC(50)) of 0.55, 0.38, and 0.34 μM, respectively, compared to...

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Veröffentlicht in:J Med Chem
Hauptverfasser: Brotherton-Pleiss, Christine, Yue, Peibin, Zhu, Yinsong, Nakamura, Kayo, Chen, Weiliang, Fu, Wenzhen, Kubota, Casie, Chen, Jasmine, Alonso-Valenteen, Felix, Mikhael, Simoun, Medina-Kauwe, Lali, Tius, Marcus A., Lopez-Tapia, Francisco, Turkson, James
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2020
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7816766/
https://ncbi.nlm.nih.gov/pubmed/33352047
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.0c01705
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