Literature DB >> 19736928

Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5).

Frederick W Goldberg1, Richard A Ward, Steven J Powell, Judit E Debreczeni, Richard A Norman, Nicola J Roberts, Allan P Dishington, Helen J Gingell, Kate F Wickson, Andrew L Roberts.   

Abstract

A novel class of 4-pyridinoxy-2-anilinopyridine-based TGF-beta type I receptor (also known as activin-like kinase 5 or ALK5) inhibitors is reported. The binding mode of this scaffold was successfully predicted by analyzing possible docked binding modes of literature inhibitors and novel synthetic ideas. Compounds such as 19 are potent ALK5 inhibitors with good physicochemical and pharmacokinetic properties and thus represent high quality leads for further optimization.

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Year:  2009        PMID: 19736928     DOI: 10.1021/jm900807w

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


  5 in total

1.  Discovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents.

Authors:  Yong Zhang; Yufen Zhao; Andrew J Tebben; Steven Sheriff; Max Ruzanov; Mark P Fereshteh; Yi Fan; Jonathan Lippy; Jesse Swanson; Ching-Ping Ho; Barri S Wautlet; Anne Rose; Karen Parrish; Zheng Yang; Andrew F Donnell; Liping Zhang; Brian E Fink; Gregory D Vite; Karen Augustine-Rauch; Joseph Fargnoli; Robert M Borzilleri
Journal:  ACS Med Chem Lett       Date:  2018-10-17       Impact factor: 4.345

2.  Structural biology of the TGFβ family.

Authors:  Erich J Goebel; Kaitlin N Hart; Jason C McCoy; Thomas B Thompson
Journal:  Exp Biol Med (Maywood)       Date:  2019-10-09

3.  Uncovering Molecular Bases Underlying Bone Morphogenetic Protein Receptor Inhibitor Selectivity.

Authors:  Abdelaziz Alsamarah; Alecander E LaCuran; Peter Oelschlaeger; Jijun Hao; Yun Luo
Journal:  PLoS One       Date:  2015-07-02       Impact factor: 3.240

4.  Structure-Based Virtual Screening, Molecular Dynamics and Binding Free Energy Calculations of Hit Candidates as ALK-5 Inhibitors.

Authors:  Sheila C Araujo; Vinicius G Maltarollo; Michell O Almeida; Leonardo L G Ferreira; Adriano D Andricopulo; Kathia M Honorio
Journal:  Molecules       Date:  2020-01-09       Impact factor: 4.411

Review 5.  Pd-Catalyzed Cross-Couplings: On the Importance of the Catalyst Quantity Descriptors, mol % and ppm.

Authors:  Christopher S Horbaczewskyj; Ian J S Fairlamb
Journal:  Org Process Res Dev       Date:  2022-07-11       Impact factor: 3.858

  5 in total

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