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1
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0028243847
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Application of combinatorial technologies to drug discovery. 1. Background and peptide combinatorial libraries
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of special interest, An in-depth perspective into the background of peptide-based chemical and biological approaches in combinatorial chemistry.
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(1994)
J Med Chem
, vol.37
, pp. 1233-1251
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Gallop1
Barrett2
Dower3
Fodor4
Gordon5
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2
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0028318863
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Applications of combinatorial technologies to drug discovery. 2. Combinatorial organic synthesis, library screening strategies, and future directions
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of special interest, A review of the literature and an analysis of problems involved in combinatorial organic synthesis and strategies for the screening of libraries. Issues that bear on the new technology are noted, and future areas of activity are suggested.
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(1994)
J Med Chem
, vol.37
, pp. 1385-1401
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Gordon1
Barrett2
Dower3
Fodor4
Gallop5
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3
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21844524973
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The challenge of preparing and testing combinatorial compound libraries in the fast lane, at the front end of drug development
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of special interest, Contains a useful appendix of terminology used in combinatorial chemistry.
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(1994)
Chimia
, vol.48
, pp. 531-541
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Felder1
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4
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15444364122
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Combinatorial drug discovery: which methods will produce the greatest value?
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(1995)
Biotechnology
, vol.13
, pp. 351-360
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Ecker1
Crooke2
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7
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0000975204
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Synthesis and applications of organic polymers as supports and protecting groups
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(1981)
Tetrahedron
, vol.37
, pp. 663-683
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Fréchet1
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10
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0027940148
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Straightforward and general method for coupling alcohols to solid supports
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of special interest, Describes a useful reagent, dihydropyran, for tethering the hydroxyl group to the bead. This is the first step for the identification of a collection of linking strategies, which will permit wide versatility in solid-phase synthetic sequences.
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(1994)
Tetrahedron Lett
, vol.35
, pp. 9333-9336
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Thompson1
Ellman2
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11
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0000246280
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Carbon—carbon bond-forming methods on solid support. Utilization of Kenner's “safety-catch” linker
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(1994)
J Am Chem Soc
, vol.116
, pp. 11171-11172
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Backes1
Ellman2
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12
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0001216513
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Reagents for combinatorial organic synthesis: development of a new o-nitrobenzyl photolabile linker for solid-phase synthesis
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of outstanding interest, Reports the development of a o-nitrobenzyl photolabile linker, a very useful reagent for releasing combinatorial libraries from beads. This photolabile linker, which is cleaved under mild conditions, capitalizes on several decades of reported literature and five years of development of photocleavable linkers for photolithographic synthesis on glass chips. In addition to the advantage of the mild cleavage conditions used, the photoproducts remaining on bead are considerably less chemically reactive than earlier linkers.
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(1995)
J Org Chem
, vol.60
, pp. 2318-2319
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Holmes1
Jones2
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13
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0029013332
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Synthesis of a small molecule combinatorial library encoded with molecular tags
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of outstanding interest, Early example of the use of an encoded synthetic library to prepare small-molecule diversity. The approach replaces the original tagging scheme [19] with an improved acylcarbene tagging method [20] and employs a photolabile linker for product release.
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(1995)
J Am Chem Soc
, vol.117
, pp. 5588-5589
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Baldwin1
Burbaum2
Henderson3
Ohlmeyer4
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16
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0029074226
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Free solution identification of candidate peptides from combinatorial libraries by affinity capillary electrophoresis/mass spectrometry
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(1995)
J Am Chem Soc
, vol.117
, pp. 5419-5420
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Chu1
Kirby2
Karger3
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18
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0029011168
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NPIT: a new reagent for quantitatively monitoring reactions of amines in combinatorial synthesis
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(1995)
Bioorg Med Chem Lett
, vol.5
, pp. 1053-1058
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Chu1
Reich2
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20
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33751157590
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A general method for molecular tagging of encoded combinatorial chemistry libraries
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of outstanding interest, Describes an improved method of inert tag encoding, relying on the reaction of acylcarbenes with the polystyrene solid support, and permitting encryption of a wide range of ligand chemistries.
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(1994)
J Org Chem
, vol.59
, pp. 4723-4724
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Nestler1
Bartlett2
Still3
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22
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0000651698
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The synthesis of phosphonate esters, and extension of the Mitsunobu reaction
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(1992)
J Org Chem
, vol.57
, pp. 6331-6335
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Campbell1
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23
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0028326599
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Phosphonate ester synthesis using a modified Mitsunobu condensation
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of outstanding interest, See [25] annotation.
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(1994)
J Org Chem
, vol.59
, pp. 658-660
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Campbell1
Bermak2
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24
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0028134093
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Solid-phase synthesis of peptidyl-phosphonates
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of outstanding interest, See [25] annotation.
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(1994)
J Am Chem Soc
, vol.116
, pp. 6039-6040
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Campbell1
Bermak2
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25
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0029076548
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A transition state analogue inhibitor combinatorial library
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of outstanding interest, This series of papers [22,23–25] shows the evolution of one of the first successful attempts at creating a small-molecule library on solid supports. The paradigm of first adapting known (solution) synthetic chemistry to solid phase, followed by application of the split synthesis procedure on beads, exemplifies the beginnings of the new approach. Newer refinements to this scheme would emphasize ‘rehearsal’ of the chemistry with a wide range of building blocks before library synthesis, monitoring of reaction progress with new analytical techniques, and mild linker release strategies.
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(1995)
J Am Chem Soc
, vol.117
, pp. 5381-5382
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Campbell1
Bermak2
Burkoth3
Patel4
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27
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0028968619
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Expedient method for the solid-phase synthesis of aspartic acid protease inhibitors directed toward the generation of libraries
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of special interest, A good example of the adaptation of organic synthesis of an important pharmacophore to solid phase, thus setting the stage for producing a hydroxyethylamine combinatorial library.
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(1995)
J Med Chem
, vol.38
, pp. 1427-1430
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Kick1
Ellman2
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28
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0029042575
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Combinatorial organic synthesis of highly functionalized pyrrolidines: identification of a potent angiotensin converting enzyme inhibitor from a mercaptoacyl proline library
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of outstanding interest, One of the first examples of creating a focused small-molecule combinatorial library using cycloaddition chemistry. Deconvolution of the library of 〉 500 mercaptoacyl proline derivatives led to the identification of a novel highly potent inhibitor of angiotensin-converting enzyme.
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(1995)
J Am Chem Soc
, vol.117
, pp. 7029-7030
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Murphy1
Schullek2
Gordon3
Gallop4
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30
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0028021332
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Post-modification of peptoid side chains: [3+2] cycloaddition of nitrile oxides with alkenes and alkynes on the solid-phase
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(1994)
Tetrahedron Lett
, vol.35
, pp. 5825-5828
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Pei1
Moos2
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32
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0028555379
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Simultaneous solid-phase synthesis of β-turn mimetics incorporating side-chain functionality
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of outstanding interest, The beginnings of integrating structure-based ligand design with combinatorial chemistry.
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(1994)
J Am Chem Soc
, vol.116
, pp. 11580-11581
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Virgilio1
Ellman2
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33
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0027068161
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A general and expedient method for the solid-phase synthesis of 1,4-benzodiazepine derivatives
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(1992)
J Am Chem Soc
, vol.114
, pp. 10997-10998
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Bunin1
Ellman2
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34
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0028278170
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The combinatorial synthesis and chemical and biological evaluation of a 1,4-benzodiazepine library
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of special interest, This is an application of the seminal work of [33], enabling solid-phase chemistry to produce one of the first combinatorial libraries of non-polymeric small molecules.
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(1994)
Proc Natl Acad Sci USA
, vol.91
, pp. 4708-4712
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Bunin1
Plunkett2
Ellman3
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35
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0028928237
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Solid-phase synthesis of structurally diverse 1,4-benzodiazepine derivatives using the Stille coupling reaction
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of special interest, The problem of a limited commercial supply of various aminobenzophenones is surmounted by devising a solid-phase combinatorial synthesis of building blocks.
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(1995)
J Am Chem Soc
, vol.117
, pp. 3306-3307
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Plunkett1
Ellman2
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37
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0028031367
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Formation of carbon—carbon bond on solid support: application of the Stille reaction
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(1994)
Tetrahedron Lett
, vol.35
, pp. 5613-5614
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Deshpande1
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41
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0000058677
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Strategies for combinatorial organic synthesis: solution- and polymer-supported synthesis of 4-thiazolidines and 4-metathiazanones derived from amino acids
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in press
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(1995)
J Org Chem
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Holmes1
Chinn2
Look3
Gordon4
Gallop5
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43
-
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0028109561
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All-cis cyclopentane scaffolding for combinatorial solid phase synthesis of small non-peptide compounds
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(1994)
Tetrahedron Letters
, vol.35
, pp. 9169-9172
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Patek1
Drake2
Lebl3
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44
-
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33748813410
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A solution-phase screening procedure for the isolation of active compounds from a library of molecules
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(1994)
Angew Chem
, vol.33
, pp. 2061-2064
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Carell1
Wintner2
Rebek3
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46
-
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0028953254
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General and efficient method for the solution- and solid-phase synthesis of vancomycin carboxamide derivatives
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(1995)
J Org Chem
, vol.60
, pp. 1102-1103
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Sundram1
Griffin2
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48
-
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0029302620
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Strategies for the synthesis and screening of glycoconjugates. 1. A library of glycosylamines
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(1995)
Bioconjugate Chem
, vol.6
, pp. 316-318
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Vetter1
Gallop2
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49
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0029005353
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The combinatorial synthesis of a 30,752-compound library: discovery of SAR around the endothelin antagonist, FR-139,317
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of special interest, A 30 000-member library of small peptidomimetics is created on the basis of a known endothelin antagonist. Strategies in which combinatorial libraries are ‘exploded’ around lead molecules will become a powerful means of evolving lead structures to meet pharmaceutical criteria.
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(1995)
Bioorg Med Chem Lett
, vol.5
, pp. 917-922
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Terrett1
Bojanic2
Brown3
Bungay4
Gardner5
Gordon6
Mayers7
Steele8
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50
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0027934780
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Discovery of nanomolar ligands for 7-transmembrane G-protein-coupled receptors from a diverse N-(substituted)glycine peptoid library
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of outstanding interest, Excellent example of the discovery of high-affinity ligands for seven-transmembrane G-protein-coupled receptors proceeding from a 5000-member library of small N-substituted glycine peptidomimetics. The library was biased to capitalize on known structure—activity relationship data, thus increasing the probability of finding a ligand by presentation of an appropriate side-chain functionality.
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(1994)
J Med Chem
, vol.37
, pp. 2678-2685
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Zuckermann1
Martin2
Spellmeyer3
Stauber4
Shoemaker5
Kerr6
Figliozzi7
Goff8
Siani9
Simon10
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51
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0028794072
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Preparation and screening against acetylcholinesterase of a non-peptide “indexed” combinatorial library
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(1995)
J Am Chem Soc
, vol.117
, pp. 1240-1245
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Pirrung1
Chen2
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