Literature DB >> 11012022

Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II.

A F Burchat1, D J Calderwood, G C Hirst, N J Holman, D N Johnston, R Munschauer, P Rafferty, G B Tometzki.   

Abstract

Pyrrolo[2,3-d]pyrimidines containing a 5-(4-phenoxyphenyl) substituent are novel, potent and selective inhibitors of lck in vitro. Exploration of C-6 position of the pyrrolo[2,3-d]pyrimidine and the terminal phenyl group structure-activity relationship (SAR) is detailed. Compound 1 is orally active in animal models.

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Year:  2000        PMID： 11012022     DOI： 10.1016/s0960-894x(00)00442-x

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  11 in total

1.  LKB1 regulates TCR-mediated PLCγ1 activation and thymocyte positive selection.

Authors:  Yonghao Cao; Hai Li; Haifeng Liu; Min Zhang; Zichun Hua; Hongbin Ji; Xiaolong Liu
Journal:  EMBO J       Date:  2011-04-12       Impact factor: 11.598

2.  Development of small molecules targeting the pseudokinase Her3.

Authors:  Sang Min Lim; Ting Xie; Kenneth D Westover; Scott B Ficarro; Hyun Seop Tae; Deepak Gurbani; Taebo Sim; Jarrod A Marto; Pasi A Jänne; Craig M Crews; Nathanael S Gray
Journal:  Bioorg Med Chem Lett       Date:  2015-05-11       Impact factor: 2.823

3.  Structural bioinformatics-based design of selective, irreversible kinase inhibitors.

Authors:  Michael S Cohen; Chao Zhang; Kevan M Shokat; Jack Taunton
Journal:  Science       Date:  2005-05-27       Impact factor: 47.728

4.  CD8+ T cell immunodominance shifts during the early stages of acute LCMV infection independently from functional avidity maturation.

Authors:  Hans-Peter Raué; Mark K Slifka
Journal:  Virology       Date:  2009-06-18       Impact factor: 3.616

5.  Binding is not enough: flexibility is needed for photocrosslinking of Lck kinase by benzophenone photoligands.

Authors:  Akira Kawamura; Sagit Hindi; Doina M Mihai; Laurence James; Olga Aminova
Journal:  Bioorg Med Chem       Date:  2008-09-03       Impact factor: 3.641

6.  Microclusters of inhibitory killer immunoglobulin-like receptor signaling at natural killer cell immunological synapses.

Authors:  Bebhinn Treanor; Peter M P Lanigan; Sunil Kumar; Chris Dunsby; Ian Munro; Egidijus Auksorius; Fiona J Culley; Marco A Purbhoo; David Phillips; Mark A A Neil; Deborah N Burshtyn; Paul M W French; Daniel M Davis
Journal:  J Cell Biol       Date:  2006-06-26       Impact factor: 10.539

7.  Pharmacological targeting of the pseudokinase Her3.

Authors:  Ting Xie; Sang Min Lim; Kenneth D Westover; Michael E Dodge; Dalia Ercan; Scott B Ficarro; Durga Udayakumar; Deepak Gurbani; Hyun Seop Tae; Steven M Riddle; Taebo Sim; Jarrod A Marto; Pasi A Jänne; Craig M Crews; Nathanael S Gray
Journal:  Nat Chem Biol       Date:  2014-10-19       Impact factor: 15.040

8.  New horizons in drug discovery of lymphocyte-specific protein tyrosine kinase (Lck) inhibitors: a decade review (2011-2021) focussing on structure-activity relationship (SAR) and docking insights.

Authors:  Ahmed Elkamhawy; Eslam M H Ali; Kyeong Lee
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

9.  In vitro membrane reconstitution of the T-cell receptor proximal signaling network.

Authors:  Enfu Hui; Ronald D Vale
Journal:  Nat Struct Mol Biol       Date:  2014-01-26       Impact factor: 15.369

Review 10.  Does B cell receptor signaling in chronic lymphocytic leukaemia cells differ from that in other B cell types?

Authors:  Joseph R Slupsky
Journal:  Scientifica (Cairo)       Date:  2014-07-02
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