Literature DB >> 10450984

Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists.

H S Ahn1, L Arik, G Boykow, D A Burnett, M A Caplen, M Czarniecki, M S Domalski, C Foster, M Manna, A W Stamford, Y Wu.   

Abstract

A series of pyrroloquinazolines has been discovered that represent novel small molecule inhibitors of the intramolecular ligand of the thrombin receptor. Analogs were prepared to study the structure-activity relationships of substitution at the N 1, N3, and N7 positions of the heterocycle. Compounds 4e and 4f have been identified with IC50's of 56 and 52 nM, respectively.

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Year:  1999        PMID: 10450984     DOI: 10.1016/s0960-894x(99)00339-x

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


  9 in total

1.  The chemistry and pharmacology of privileged pyrroloquinazolines.

Authors:  Bo Chao; Bingbing X Li; Xiangshu Xiao
Journal:  Medchemcomm       Date:  2015-04-01       Impact factor: 3.597

2.  Linking High-Throughput Screens to Identify MoAs and Novel Inhibitors of Mycobacterium tuberculosis Dihydrofolate Reductase.

Authors:  John P Santa Maria; Yumi Park; Lihu Yang; Nicholas Murgolo; Michael D Altman; Paul Zuck; Greg Adam; Chad Chamberlin; Peter Saradjian; Peter Dandliker; Helena I M Boshoff; Clifton E Barry; Charles Garlisi; David B Olsen; Katherine Young; Meir Glick; Elliott Nickbarg; Peter S Kutchukian
Journal:  ACS Chem Biol       Date:  2017-08-29       Impact factor: 5.100

3.  Design, synthesis and evaluation of antitumor acylated monoaminopyrroloquinazolines.

Authors:  Bo Chao; Bingbing X Li; Xiangshu Xiao
Journal:  Bioorg Med Chem Lett       Date:  2017-05-16       Impact factor: 2.823

Review 4.  Targeting PAR1: Now What?

Authors:  Robert Flaumenhaft; Karen De Ceunynck
Journal:  Trends Pharmacol Sci       Date:  2017-05-27       Impact factor: 14.819

5.  Thrombin-induced conversion of fibrinogen to fibrin results in rapid platelet trapping which is not dependent on platelet activation or GPIb.

Authors:  Gavin E Jarvis; Ben T Atkinson; Jon Frampton; Steve P Watson
Journal:  Br J Pharmacol       Date:  2003-02       Impact factor: 8.739

6.  Protease-activated receptor-1 (PAR-1) promotes the motility of human melanomas and is associated to their metastatic phenotype.

Authors:  Antonietta Silini; Carmen Ghilardi; Camilla Ardinghi; Sergio Bernasconi; Paolo Oliva; Fabio Carraro; Antonella Naldini; Maria Rosa Bani; Raffaella Giavazzi
Journal:  Clin Exp Metastasis       Date:  2009-12-20       Impact factor: 5.150

7.  Discovery of a Potent Anti-tumor Agent through Regioselective Mono-N-acylation of 7H-Pyrrolo[3,2-f]quinazoline-1,3-diamine.

Authors:  Jingjin Chen; Alina Kassenbrock; Bingbing X Li; Xiangshu Xiao
Journal:  Medchemcomm       Date:  2013-09-01       Impact factor: 3.597

8.  Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.

Authors:  Chris Dockendorff; Omozuanvbo Aisiku; Lynn Verplank; James R Dilks; Daniel A Smith; Susanna F Gunnink; Louisa Dowal; Joseph Negri; Michelle Palmer; Lawrence Macpherson; Stuart L Schreiber; Robert Flaumenhaft
Journal:  ACS Med Chem Lett       Date:  2012-01-30       Impact factor: 4.345

9.  Novel 2,3-Dihydro-1H-pyrrolo[3,2,1-ij]quinazolin-1-ones: Synthesis and Biological Evaluation.

Authors:  Malose J Mphahlele; Tebogo A Khoza; Peaceful Mabeta
Journal:  Molecules       Date:  2016-12-30       Impact factor: 4.411

  9 in total

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