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Novel potent azetidine-based compounds irreversibly inhibit Stat3 activation and induce antitumor response against human breast tumor growth in vivo.
Yue P, Zhu Y, Brotherton-Pleiss C, Fu W, Verma N, Chen J, Nakamura K, Chen W, Chen Y, Alonso-Valenteen F, Mikhael S, Medina-Kauwe L, Kershaw KM, Celeridad M, Pan S, Limpert AS, Sheffler DJ, Cosford NDP, Shiao SL, Tius MA, Lopez-Tapia F, Turkson J. Yue P, et al. Among authors: tius ma. Cancer Lett. 2022 May 28;534:215613. doi: 10.1016/j.canlet.2022.215613. Epub 2022 Mar 9. Cancer Lett. 2022. PMID: 35276290 Free PMC article.
Linker Variation and Structure-Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors.
Lopez-Tapia F, Brotherton-Pleiss C, Yue P, Murakami H, Costa Araujo AC, Reis Dos Santos B, Ichinotsubo E, Rabkin A, Shah R, Lantz M, Chen S, Tius MA, Turkson J. Lopez-Tapia F, et al. Among authors: tius ma. ACS Med Chem Lett. 2018 Feb 16;9(3):250-255. doi: 10.1021/acsmedchemlett.7b00544. eCollection 2018 Mar 8. ACS Med Chem Lett. 2018. PMID: 29541369 Free PMC article.
Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors.
Brotherton-Pleiss C, Yue P, Zhu Y, Nakamura K, Chen W, Fu W, Kubota C, Chen J, Alonso-Valenteen F, Mikhael S, Medina-Kauwe L, Tius MA, Lopez-Tapia F, Turkson J. Brotherton-Pleiss C, et al. Among authors: tius ma. J Med Chem. 2021 Jan 14;64(1):695-710. doi: 10.1021/acs.jmedchem.0c01705. Epub 2020 Dec 22. J Med Chem. 2021. PMID: 33352047 Free PMC article.
Azetidine ring, salicylic acid, and salicylic acid bioisosteres as determinants of the binding characteristics of novel potent compounds to Stat3.
Chen Y, Zhai N, Zhu Y, Yue P, Verma N, Brotherton-Pleiss C, Fu W, Nakamura K, Chen W, Kawakami J, Murali R, Tius MA, Lopez-Tapia F, Turkson J. Chen Y, et al. Among authors: tius ma. Bioorg Med Chem Lett. 2024 Jan 1;97:129565. doi: 10.1016/j.bmcl.2023.129565. Epub 2023 Nov 24. Bioorg Med Chem Lett. 2024. PMID: 38008341 Free article. No abstract available.
Convergent cyclopentannelation process.
Bee C, Tius MA. Bee C, et al. Among authors: tius ma. Org Lett. 2003 May 15;5(10):1681-4. doi: 10.1021/ol034309+. Org Lett. 2003. PMID: 12735751
73 results