Literature DB >> 12852972

Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors.

Jagabandhu Das1, Robert V Moquin, James Lin, Chunjian Liu, Arthur M Doweyko, Henry F DeFex, Qiong Fang, Suhong Pang, Sidney Pitt, Ding Ren Shen, Gary L Schieven, Joel C Barrish, John Wityak.   

Abstract

A series of structurally novel benzothiazole based small molecule inhibitors of p56(lck) was prepared to elucidate their structure-activity relationships (SAR), selectivity and cell activity in the T-cell proliferation assay. BMS-350751 (2) and BMS-358233 (3) are identified as potent Lck inhibitors with excellent cellular activities against T-cell proliferation.

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Year:  2003        PMID: 12852972     DOI: 10.1016/s0960-894x(03)00511-0

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


  6 in total

1.  Discovery and characterization of potent thiazoles versus methicillin- and vancomycin-resistant Staphylococcus aureus.

Authors:  Haroon Mohammad; Abdelrahman S Mayhoub; Adil Ghafoor; Muhammad Soofi; Ruba A Alajlouni; Mark Cushman; Mohamed N Seleem
Journal:  J Med Chem       Date:  2014-01-14       Impact factor: 7.446

2.  RITA Mimics: Synthesis and Mechanistic Evaluation of Asymmetric Linked Trithiazoles.

Authors:  Adrian L Pietkiewicz; Yuqi Zhang; Marwa N Rahimi; Michael Stramandinoli; Matthew Teusner; Shelli R McAlpine
Journal:  ACS Med Chem Lett       Date:  2017-03-06       Impact factor: 4.345

3.  Anti-biofilm activity and synergism of novel thiazole compounds with glycopeptide antibiotics against multidrug-resistant staphylococci.

Authors:  Haroon Mohammad; Abdelrahman S Mayhoub; Mark Cushman; Mohamed N Seleem
Journal:  J Antibiot (Tokyo)       Date:  2014-10-15       Impact factor: 2.649

4.  Antimicrobial prospect of newly synthesized 1,3-thiazole derivatives.

Authors:  Bassem Sadek; Moawia Mohammad Al-Tabakha; Khairi Mustafa Salem Fahelelbom
Journal:  Molecules       Date:  2011-11-09       Impact factor: 4.411

5.  (2E)-2-(1,3-Benzo-thia-zol-2-yl)-3-(di-methyl-amino)-prop-2-ene-nitrile.

Authors:  Shaaban K Mohamed; Mehmet Akkurt; Benson M Kariuki; Ali M Ali; Mustafa R Albayati
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-12-14

Review 6.  Recent Advances in Synthesis of Benzothiazole Compounds Related to Green Chemistry.

Authors:  Xiang Gao; Jiao Liu; Xin Zuo; Xinyue Feng; Ying Gao
Journal:  Molecules       Date:  2020-04-05       Impact factor: 4.411

  6 in total

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