Literature DB >> 8804539

A solution-phase strategy for the synthesis of chemical libraries containing small organic molecules: a universal and dipeptide mimetic template.

S Cheng1, C M Tarby, D D Comer, J P Williams, L H Caporale, P L Myers, D L Boger.   

Abstract

A general approach to the solution phase, parallel synthesis of chemical libraries, which allows the preparation of multi-milligram quantities of each individual member, is exemplified with both a universal and dipeptide mimetic template. In each step of the sequence, the reactants, unreacted starting material, reagents and their byproducts are removed by simple liquid/ liquid or liquid/solid extractions providing the desired intermediates and final compounds in high purities (> or = 90-100%) independent of the reaction yields and without deliberate reaction optimization.

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Year:  1996        PMID: 8804539     DOI: 10.1016/0968-0896(96)00069-7

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  15 in total

1.  Identification of broad-based HIV-1 protease inhibitors from combinatorial libraries.

Authors:  Max W Chang; Michael J Giffin; Rolf Muller; Jeremiah Savage; Ying C Lin; Sukwon Hong; Wei Jin; Landon R Whitby; John H Elder; Dale L Boger; Bruce E Torbett
Journal:  Biochem J       Date:  2010-08-01       Impact factor: 3.857

2.  Synthesis and evaluation of duocarmycin SA analogs incorporating the methyl 1,2,8,8a-tetrahydrocyclopropa[c]oxazolo[2,3-e]indol-4-one-6-carboxylate (COI) alkylation subunit.

Authors:  Kristopher E Boyle; Karen S MacMillan; David A Ellis; James P Lajiness; William M Robertson; Dale L Boger
Journal:  Bioorg Med Chem Lett       Date:  2010-02-02       Impact factor: 2.823

3.  Discovery of inhibitors of aberrant gene transcription from Libraries of DNA binding molecules: inhibition of LEF-1-mediated gene transcription and oncogenic transformation.

Authors:  James S Stover; Jin Shi; Wei Jin; Peter K Vogt; Dale L Boger
Journal:  J Am Chem Soc       Date:  2009-03-11       Impact factor: 15.419

4.  Discovery of HIV fusion inhibitors targeting gp41 using a comprehensive α-helix mimetic library.

Authors:  Landon R Whitby; Kristopher E Boyle; Lifeng Cai; Xiaoqian Yu; Miriam Gochin; Dale L Boger
Journal:  Bioorg Med Chem Lett       Date:  2012-03-03       Impact factor: 2.823

5.  Inhibition of adenovirus replication by a trisubstituted piperazin-2-one derivative.

Authors:  Javier Sanchez-Cespedes; Crystal L Moyer; Landon R Whitby; Dale L Boger; Glen R Nemerow
Journal:  Antiviral Res       Date:  2014-06-04       Impact factor: 5.970

6.  Design, synthesis, and validation of a β-turn mimetic library targeting protein-protein and peptide-receptor interactions.

Authors:  Landon R Whitby; Yoshio Ando; Vincent Setola; Peter K Vogt; Bryan L Roth; Dale L Boger
Journal:  J Am Chem Soc       Date:  2011-06-15       Impact factor: 15.419

7.  Small molecule peptidomimetic inhibitors of importin α/β mediated nuclear transport.

Authors:  Géza Ambrus; Landon R Whitby; Eric L Singer; Oleg Trott; Euna Choi; Arthur J Olson; Dale L Boger; Larry Gerace
Journal:  Bioorg Med Chem       Date:  2010-08-21       Impact factor: 3.641

8.  Discovery libraries targeting the major enzyme classes: the serine hydrolases.

Authors:  Katerina Otrubova; Venkat Srinivasan; Dale L Boger
Journal:  Bioorg Med Chem Lett       Date:  2014-06-27       Impact factor: 2.823

9.  Characterization of lassa virus cell entry inhibitors: determination of the active enantiomer by asymmetric synthesis.

Authors:  Landon R Whitby; Andrew M Lee; Stefan Kunz; Michael B A Oldstone; Dale L Boger
Journal:  Bioorg Med Chem Lett       Date:  2009-05-03       Impact factor: 2.823

10.  Unique small molecule entry inhibitors of hemorrhagic fever arenaviruses.

Authors:  Andrew M Lee; Jillian M Rojek; Christina F Spiropoulou; Anette T Gundersen; Wei Jin; Alex Shaginian; Joanne York; Jack H Nunberg; Dale L Boger; Michael B A Oldstone; Stefan Kunz
Journal:  J Biol Chem       Date:  2008-05-12       Impact factor: 5.157

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