Literature DB >> 23350847

Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.

Fernando Padilla1, Niala Bhagirath, Shaoqing Chen, Eric Chiao, David M Goldstein, Johannes C Hermann, Jonathan Hsu, Joshua J Kennedy-Smith, Andreas Kuglstatter, Cheng Liao, Wenjian Liu, Lee E Lowrie, Kin Chun Luk, Stephen M Lynch, John Menke, Linghao Niu, Timothy D Owens, Counde O-Yang, Aruna Railkar, Ryan C Schoenfeld, Michelle Slade, Sandra Steiner, Yun-Chou Tan, Armando G Villaseñor, Ce Wang, Jutta Wanner, Wenwei Xie, Daigen Xu, Xiaohu Zhang, Mingyan Zhou, Matthew C Lucas.   

Abstract

We describe the discovery of several pyrrolopyrazines as potent and selective Syk inhibitors and the efforts that eventually led to the desired improvements in physicochemical properties and human whole blood potencies. Ultimately, our mouse model revealed unexpected toxicity that precluded us from further advancing this series.

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Year:  2013        PMID: 23350847     DOI: 10.1021/jm301720p

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  7 in total

1.  Synthesis, biological evaluation and mechanism studies of matrine derivatives as anticancer agents.

Authors:  Lihe Jiang; Lichuan Wu; Fangfang Yang; Nadin Almosnid; Xu Liu; Jun Jiang; Elliot Altman; Lisheng Wang; Ying Gao
Journal:  Oncol Lett       Date:  2017-06-23       Impact factor: 2.967

2.  3D-QSAR-Based Pharmacophore Modeling, Virtual Screening, and Molecular Dynamics Simulations for the Identification of Spleen Tyrosine Kinase Inhibitors.

Authors:  Vikas Kumar; Shraddha Parate; Amir Zeb; Pooja Singh; Gihwan Lee; Tae Sung Jung; Keun Woo Lee; Min Woo Ha
Journal:  Front Cell Infect Microbiol       Date:  2022-06-30       Impact factor: 6.073

3.  Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases.

Authors:  Peter Blomgren; Jayaraman Chandrasekhar; Julie A Di Paolo; Wanchi Fung; Guoju Geng; Carmen Ip; Randall Jones; Jeffrey E Kropf; Eric B Lansdon; Seung Lee; Jennifer R Lo; Scott A Mitchell; Bernard Murray; Chris Pohlmeyer; Aaron Schmitt; Kimberly Suekawa-Pirrone; Sarah Wise; Jin-Ming Xiong; Jianjun Xu; Helen Yu; Zhongdong Zhao; Kevin S Currie
Journal:  ACS Med Chem Lett       Date:  2020-02-12       Impact factor: 4.345

4.  A combined experimental and computational study of Vam3, a derivative of resveratrol, and Syk interaction.

Authors:  Ming Jiang; Renping Liu; Ying Chen; Qisheng Zheng; Saijun Fan; Peixun Liu
Journal:  Int J Mol Sci       Date:  2014-09-25       Impact factor: 5.923

5.  Targeted inhibition of Polo-like kinase 1 by a novel small-molecule inhibitor induces mitotic catastrophe and apoptosis in human bladder cancer cells.

Authors:  Zhe Zhang; Guojun Zhang; Chuize Kong
Journal:  J Cell Mol Med       Date:  2016-11-23       Impact factor: 5.310

6.  Characterizing the structure-activity relationships of natural products, tanshinones, reveals their mode of action in inhibiting spleen tyrosine kinase.

Authors:  Min-Che Tung; Keng-Chang Tsai; Kit-Man Fung; Ming-Jaw Don; Tien-Sheng Tseng
Journal:  RSC Adv       Date:  2021-01-14       Impact factor: 3.361

7.  Syk Inhibitors: New Computational Insights into Their Intraerythrocytic Action in Plasmodium falciparum Malaria.

Authors:  Giuseppe Marchetti; Alessandro Dessì; Roberto Dallocchio; Ioannis Tsamesidis; Maria Carmina Pau; Francesco Michelangelo Turrini; Antonella Pantaleo
Journal:  Int J Mol Sci       Date:  2020-09-23       Impact factor: 5.923

  7 in total

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