Výsledky vyhledávání

Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors

Autor: Martin Dolmaski, Brandon M. Taoka, Jared N. Cumming, Maria S. Michener, Lynn A. Hyde, Jinsong Hao, Brad E. Smith, Hongwu Wang, Wen-Lian Wu, Matthew E. Kennedy, Dorthy Levorse, Peter Orth, Eric M. Parker

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 56:128463

This paper describes the structure-activity-relationships of novel fluoroalkyl substituents at the C2 position of iminothiazine dioxide beta secretase inhibitors. Key discoveries include reduced amidine basicity and its effect on Pgp, cell potency, a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::984b2c3cec4c248c956651aadfe2ea29
https://doi.org/10.1016/j.bmcl.2021.128463

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Abstract 1145: AGX323 - A SAM-competitive, orally available inhibitor of protein arginine methyltransferase 5 (PRMT5) with potent cellular antiproliferative and in vivo antitumor activity against selected solid cancer types

Autor: Wen-Lian Wu, Francis Y.F. Lee, Yang Zhiqiang, Tan John Qiang

Publikováno v: Cancer Research. 81:1145-1145

Background: Protein arginine methyltransferase 5 (PRMT5) is an attractive therapeutic target because of its involvement in key oncogenic mechanisms including epigenetics, DNA response and RNA processing. Early development of PRMT5 inhibitors has focu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8e138572711ebcbdb4272229004d0162
https://doi.org/10.1158/1538-7445.am2021-1145

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Abstract 1286: AGX87 - An IND-stage potent and selective next-generation NTRK/ROS1 inhibitor of WT and clinical resistant mutants with superiority over tyrosine kinase inhibitors currently approved or in development

Autor: Tan John Qiang, Yang Zhiqiang, Wen-Lian Wu, Francis Y.F. Lee

Publikováno v: Cancer Research. 81:1286-1286

AGX87 - An IND-stage potent and selective next-generation NTRK/ROS1 inhibitor of WT and clinical resistant mutants with superiority over tyrosine kinase inhibitors currently approved or in development Background: Fusions of the neurotrophic receptor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::50433ee7237556489f7cb1b59391d517
https://doi.org/10.1158/1538-7445.am2021-1286

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Scaffold-hopping from xanthines to tricyclic guanines: A case study of dipeptidyl peptidase 4 (DPP4) inhibitors

Autor: Theresa M. Kelly, John W. Clader, Dmitri A. Pissarnitski, Johannes H. Voigt, Duane A. Burnett, David Cole, Giovanna Scapin, Wen-Lian Wu, Zuliang Yao, Aileen Soriano, Zhiqiang Zhao, Martin S. Domalski, Mary Ann Powles

Publikováno v: Bioorganic & Medicinal Chemistry. 24:5534-5545

Molecular modeling of unbound tricyclic guanine scaffolds indicated that they can serve as effective bioisosteric replacements of xanthines. This notion was further confirmed by a combination of X-ray crystallography and SAR studies, indicating that

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b96060e96c9a81fdd52198d4a12ca14
https://doi.org/10.1016/j.bmc.2016.09.007

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A novel domino reaction for the preparation of substituted non-racemic β-proline derivatives

Autor: Hong Liu, Shawn P. Walsh, Yan Qi, Jiaqiang Cai, Jack D. Scott, Xin-Jie Chu, Cuizhi Mu, Brandon M. Taoka, Yaxian Cai, Jinsong Hao, Quang Truong, Zhong Lai, Xing Dai, Wen-Lian Wu, Jeffrey T. Kuethe, Eric J. Gilbert, Andrew Brunskill, Jared N. Cumming

Publikováno v: Tetrahedron. 72:6011-6020

A novel domino reaction for the preparation of non-racemic β-proline derivatives is reported. The addition of a methyl 2-(oxetan-3-yl)acetate titanium enolate to chiral tert-butanesulfinyl ketimines followed by an intramolecular oxetane ring-opening

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4f6ea7d457ba02cc5aae8322fdf057d3
https://doi.org/10.1016/j.tet.2016.08.017

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Abstract 1942: AGX73 is an effective treatment for hepatocellular carcinoma (HCC) by selective inhibition of immunokinases that play crucial roles in the crosstalk between cancer and immune cells in the tumor microenvironment

Autor: Yang Zhiqiang, Tan John Qiang, Francis Y.F. Lee, Wen-Lian Wu

Publikováno v: Cancer Research. 80:1942-1942

HCC is the second leading cause of cancer-related death and the fifth-most-common cancer worldwide. Unlike almost all other tumor types, the vast majority (90%) of HCCs develop due to underlying chronic inflammation, the induction of fibrosis and/or

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7d48659276853377bc00e6c76b80b031
https://doi.org/10.1158/1538-7445.am2020-1942

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Diversity-Oriented Synthesis through Rh-Catalyzed Selective Transformations of a Novel Multirole Directing Group

Autor: Wen-lian Wu, Bo Su, Zhang-Jie Shi, Jiangbo Wei

Publikováno v: ChemCatChem. 7:2986-2990

The Rh-catalyzed reaction of N-phthalimidyl benzamides (I) with diaryl alkynes (II) in the presence of Cu(O-Ac)2 and O2 leads to N-phthalimidyl 3,4-diarylisoquinolinones (III), whilst the reaction in the presence of cesium acetate under nitrogen give

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https://doi.org/10.1002/cctc.201500410

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Abstract C082: AGX-73, a novel small molecule multi-immunokinase inhibitor, has robust antitumor activity in murine syngeneic tumor models as a single agent and in combination with anti-PD1 checkpoint inhibitor

Autor: Tan John Qiang, Francis Y.F. Lee, Yang Zhiqiang, Wen-Lian Wu

Publikováno v: Molecular Cancer Therapeutics. 18:C082-C082

One of the central hypotheses of modern targeted cancer treatment paradigm is that aberrant activation and/or over-expression of oncogenic kinases drive intrinsic cancer cell proliferation and survival and is the causative event in cancer initiation

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::85a3a0dc9c27e1092d49c5350e3ef79c
https://doi.org/10.1158/1535-7163.targ-19-c082

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Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:844-849

An investigation is detailed of the structure activity relationships (SAR) of two sulfone side chains of compound (−)- 1a (SCH 900229), a potent, PS1-selective γ-secretase inhibitor and clinical candidate for the treatment of Alzheimer’s disease

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d7acb8f10ab43bcf5cd40b91f4b39ca
https://doi.org/10.1016/j.bmcl.2012.11.047

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