Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors
[Display omitted] In an in-house screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and synthesized, among which some compounds had potent TNIK inhibition with IC50 values lower than 1 nM. Some compounds showed concentra...
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| Published in | Bioorganic & medicinal chemistry letters Vol. 33; p. 127749 |
|---|---|
| Main Authors | , , , , , , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
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01.02.2021
Elsevier |
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| Abstract | [Display omitted]
In an in-house screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and synthesized, among which some compounds had potent TNIK inhibition with IC50 values lower than 1 nM. Some compounds showed concentration-dependent characteristics of IL-2 inhibition. These results provided new applications of TNIK inhibitors and new prospects of TNIK as a drug target. |
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| AbstractList | In an in-house screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and synthesized, among which some compounds had potent TNIK inhibition with IC
values lower than 1 nM. Some compounds showed concentration-dependent characteristics of IL-2 inhibition. These results provided new applications of TNIK inhibitors and new prospects of TNIK as a drug target. [Display omitted] In an in-house screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and synthesized, among which some compounds had potent TNIK inhibition with IC50 values lower than 1 nM. Some compounds showed concentration-dependent characteristics of IL-2 inhibition. These results provided new applications of TNIK inhibitors and new prospects of TNIK as a drug target. In an in-house screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and synthesized, among which some compounds had potent TNIK inhibition with IC50 values lower than 1 nM. Some compounds showed concentration-dependent characteristics of IL-2 inhibition. These results provided new applications of TNIK inhibitors and new prospects of TNIK as a drug target. |
| ArticleNumber | 127749 |
| Author | Miao, Zehong Yang, Bowen Wang, Yingqing Wang, Xin Chen, Lin Liu, Tongchao Xiong, Bing Yang, Yueyue Zhao, Dongmei Wu, Qian Chen, Danqi Sun, Yin Huan, Xiajuan |
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| Cites_doi | 10.1038/emboj.2009.285 10.1016/j.bmcl.2019.05.032 10.1038/cddis.2016.97 10.1074/jbc.M406370200 10.1371/journal.pbio.1001376 10.1038/s41467-020-15413-7 10.1371/journal.pone.0110180 10.1016/j.bmcl.2012.11.013 10.1038/ncomms12586 |
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| References_xml | – volume: 279 start-page: 49488 year: 2004 end-page: 49496 ident: b0005 article-title: The Traf2- and Nck-interacting kinase as a putative effector of Rap2 to regulate actin cytoskeleton publication-title: J Biol Chem contributor: fullname: Takei – volume: 11 start-page: 1632 year: 2020 end-page: 1647 ident: b0020 article-title: TNIK signaling imprints CD8(+) T cell memory formation early after priming publication-title: Nat Commun contributor: fullname: Hopner – volume: 9 year: 2014 ident: b0035 article-title: A novel aminothiazole KY-05009 with potential to inhibit Traf2- and Nck-interacting kinase (TNIK) attenuates TGF-beta1-mediated epithelial-to-mesenchymal transition in human lung adenocarcinoma A549 cells publication-title: PLoS ONE contributor: fullname: Kim – volume: 7 start-page: 12586 year: 2016 end-page: 12599 ident: b0025 article-title: TNIK inhibition abrogates colorectal cancer stemness publication-title: Nat Commun contributor: fullname: Ohbayashi – volume: 28 start-page: 3329 year: 2009 end-page: 3340 ident: b0015 article-title: The kinase TNIK is an essential activator of Wnt target genes publication-title: EMBO J contributor: fullname: Ng – volume: 23 start-page: 569 year: 2013 end-page: 573 ident: b0040 article-title: Discovery of 4-phenyl-2-phenylaminopyridine based TNIK inhibitors publication-title: Bioorg Med Chem Lett contributor: fullname: Yuan – volume: 7 year: 2016 ident: b0045 article-title: Cell cycle and apoptosis regulation by NFAT transcription factors: new roles for an old player publication-title: Cell Death Dis contributor: fullname: Viola – volume: 29 start-page: 1962 year: 2019 end-page: 1967 ident: b0030 article-title: Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase publication-title: Bioorg Med Chem Lett contributor: fullname: Nguyen-McCarty – volume: 28 start-page: 3329 year: 2009 ident: WOS:000271891400006 article-title: The kinase TNIK is an essential activator of Wnt target genes publication-title: EMBO JOURNAL doi: 10.1038/emboj.2009.285 contributor: fullname: Mahmoudi, T – volume: 29 start-page: 1962 year: 2019 ident: WOS:000471750200020 article-title: Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase publication-title: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS doi: 10.1016/j.bmcl.2019.05.032 contributor: fullname: Read, J – volume: 7 start-page: ARTN e2199 year: 2016 ident: WOS:000375277600026 article-title: Cell cycle and apoptosis regulation by NFAT transcription factors: new roles for an old player publication-title: CELL DEATH & DISEASE doi: 10.1038/cddis.2016.97 contributor: fullname: Mognol, GP – volume: 279 start-page: 49488 year: 2004 ident: WOS:000225098100119 article-title: The Traf2- and Nck-interacting kinase as a putative effector of Rap2 to regulate actin cytoskeleton publication-title: JOURNAL OF BIOLOGICAL CHEMISTRY doi: 10.1074/jbc.M406370200 contributor: fullname: Taira, K – volume: 10 start-page: ARTN e1001376 year: 2012 ident: WOS:000308501400004 article-title: The Germinal Center Kinase TNIK Is Required for Canonical NF-kappa B and JNK Signaling in B-Cells by the EBV Oncoprotein LMP1 and the CD40 Receptor publication-title: PLOS BIOLOGY doi: 10.1371/journal.pbio.1001376 contributor: fullname: Shkoda, A – volume: 11 start-page: ARTN 1632 year: 2020 ident: WOS:000525081200008 article-title: TNIK signaling imprints CD8(+) T cell memory formation early after priming publication-title: NATURE COMMUNICATIONS doi: 10.1038/s41467-020-15413-7 contributor: fullname: Jaeger-Ruckstuhl, CA – volume: 9 start-page: ARTN e110180 year: 2014 ident: WOS:000343674800028 article-title: A Novel Aminothiazole KY-05009 with Potential to Inhibit Traf2-and Nck-Interacting Kinase (TNIK) Attenuates TGF-beta 1-Mediated Epithelial-to-Mesenchymal Transition in Human Lung Adenocarcinoma A549 Cells publication-title: PLOS ONE doi: 10.1371/journal.pone.0110180 contributor: fullname: Kim, J – volume: 23 start-page: 569 year: 2013 ident: WOS:000312959600038 article-title: Discovery of 4-phenyl-2-phenylaminopyridine based TNIK inhibitors publication-title: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS doi: 10.1016/j.bmcl.2012.11.013 contributor: fullname: Ho, KK – volume: 7 start-page: ARTN 12586 year: 2016 ident: WOS:000383739000001 article-title: TNIK inhibition abrogates colorectal cancer stemness publication-title: NATURE COMMUNICATIONS doi: 10.1038/ncomms12586 contributor: fullname: Masuda, M – volume: 29 start-page: 1962 issue: 15 year: 2019 ident: 10.1016/j.bmcl.2020.127749_b0030 article-title: Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase publication-title: Bioorg Med Chem Lett doi: 10.1016/j.bmcl.2019.05.032 contributor: fullname: Read – volume: 7 start-page: 12586 year: 2016 ident: 10.1016/j.bmcl.2020.127749_b0025 article-title: TNIK inhibition abrogates colorectal cancer stemness publication-title: Nat Commun doi: 10.1038/ncomms12586 contributor: fullname: Masuda – volume: 23 start-page: 569 issue: 2 year: 2013 ident: 10.1016/j.bmcl.2020.127749_b0040 article-title: Discovery of 4-phenyl-2-phenylaminopyridine based TNIK inhibitors publication-title: Bioorg Med Chem Lett doi: 10.1016/j.bmcl.2012.11.013 contributor: fullname: Ho – volume: 279 start-page: 49488 issue: 47 year: 2004 ident: 10.1016/j.bmcl.2020.127749_b0005 article-title: The Traf2- and Nck-interacting kinase as a putative effector of Rap2 to regulate actin cytoskeleton publication-title: J Biol Chem doi: 10.1074/jbc.M406370200 contributor: fullname: Taira – volume: 11 start-page: 1632 issue: 1 year: 2020 ident: 10.1016/j.bmcl.2020.127749_b0020 article-title: TNIK signaling imprints CD8(+) T cell memory formation early after priming publication-title: Nat Commun doi: 10.1038/s41467-020-15413-7 contributor: fullname: Jaeger-Ruckstuhl – volume: 9 issue: 10 year: 2014 ident: 10.1016/j.bmcl.2020.127749_b0035 article-title: A novel aminothiazole KY-05009 with potential to inhibit Traf2- and Nck-interacting kinase (TNIK) attenuates TGF-beta1-mediated epithelial-to-mesenchymal transition in human lung adenocarcinoma A549 cells publication-title: PLoS ONE doi: 10.1371/journal.pone.0110180 contributor: fullname: Kim – ident: 10.1016/j.bmcl.2020.127749_b0010 doi: 10.1371/journal.pbio.1001376 – volume: 28 start-page: 3329 issue: 21 year: 2009 ident: 10.1016/j.bmcl.2020.127749_b0015 article-title: The kinase TNIK is an essential activator of Wnt target genes publication-title: EMBO J doi: 10.1038/emboj.2009.285 contributor: fullname: Mahmoudi – volume: 7 issue: 4 year: 2016 ident: 10.1016/j.bmcl.2020.127749_b0045 article-title: Cell cycle and apoptosis regulation by NFAT transcription factors: new roles for an old player publication-title: Cell Death Dis doi: 10.1038/cddis.2016.97 contributor: fullname: Mognol |
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In an in-house screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were... In an in-house screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and... |
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| SubjectTerms | 1H-pyrrolo[2,3-b]pyridine Chemistry Chemistry, Medicinal Chemistry, Organic IL-2 secretion inhibitory Life Sciences & Biomedicine Pharmacology & Pharmacy Physical Sciences Science & Technology TNIK inhibitor |
| Title | Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors |
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