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  • 1
    Electronic Resource
    Electronic Resource
    Melanin concentrating hormone analogs: contraction of the cyclic structure. 1. Agonist activity (1988)
    s.l. : American Chemical Society
    Journal of medicinal chemistry 31 (1988), S. 949-954 
    Details
    ISSN: 1520-4804
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/jm00400a010
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  • 2
    Electronic Resource
    Electronic Resource
    Design considerations and computer modeling related to the development of molecular scaffolds and peptide mimetics for combinatorial chemistry (1996)
    Springer
    Molecular diversity 2 (1996), S. 46-56 
    Details
    ISSN: 1573-501X
    Keywords: Scaffold design ; Backbone conformation ; Topography ; Chi space ; Topographical design
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary A critical issue in drug discovery utilizing combinatorial chemistry as part of the discovery process is the choice of scaffolds to be used for a proper presentation, in a three-dimensional space, of the critical elements of structure necessary for molecular recognition (binding) and information transfer (agonist/ antagonist). In the case of polypeptide ligands, considerations related to the properties of various backbone structures (α-helix, β-sheets, etc.; φ, ψ space) and those related to three-dimensional presentation of side-chain moieties (topography; χ (chi) space) must be addressed, although they often present quite different elements in the molecular recognition puzzle. We have addressed aspects of this problem by examining the three-dimensional structures of chemically different scaffolds at various distances from the scaffold to evaluate their putative diversity. We find that chemically diverse scaffolds can readily become topographically similar. We suggest a topographical approach involving design in chi space to deal with these problems.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01718700
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  • 3
    Electronic Resource
    Electronic Resource
    Structurally homogeneous and heterogeneous synthetic combinatorial libraries (1996)
    Springer
    Molecular diversity 1 (1996), S. 149-164 
    Details
    ISSN: 1573-501X
    Keywords: Combinatorial chemistry ; Library ; Scaffold ; Solid-phase synthesis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary We have designed and synthesized structurally homogeneous and heterogeneous nonpeptide libraries. Structurally homogeneous libraries are characterized by the presence of one common structural unit, a scaffold, in all library compounds (e.g. cyclopentane, cyclohexane, diketopiperazine, thiazolidine). In structurally heterogeneous libraries different organic reactions (acylation, etherification, reductive amination, nucleophilic displacement) were applied to connect bifunctional building blocks unrelated in structure (aromatic hydroxy acids, aromatic hydroxy aldehydes, amino alcohols, diamines, and amino acids). The focus of this communication is to document the use of bifunctional building blocks for the design and synthesis of structurally heterogeneous libraries ofN-(alkoxy acyl)amino acids, N,N′-bis-(alkoxy acyl)diamino acids,N-acylamino ethers,N-(alkoxy acyl)amino alcohols,N-alkylamino ethers, andN-(alkoxy aryl)diamines.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01544953
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  • 4
    Electronic Resource
    Electronic Resource
    Synthetic library techniques: Subjective (biased and generic) thoughts and views (1996)
    Springer
    Molecular diversity 1 (1996), S. 193-216 
    Details
    ISSN: 1573-501X
    Keywords: Synthetic libraries ; Peptide libraries ; One-bead-one-compound libraries ; Deconvolution ; Diversity ; Screening approaches
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary Various aspects of synthetic diversity generation and screening are discussed. Controversial issues are raised and different points of view are presented. We hope the article will stimulate thinking about the utilization of library techniques and start a discussion about questions concerning their application.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01544958
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  • 5
    Electronic Resource
    Electronic Resource
    New approach for preparation of 2,3,7-trisubstituted 3,4-dihydroisoquinolinone libraries on solid phase (2000)
    Springer
    Molecular diversity 5 (2000), S. 153-161 
    Details
    ISSN: 1573-501X
    Keywords: decarboxylation ; dihydroisoquinoline ; solid phase
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract In an attempt to prepare 7-substituted 3,4-dihydroisoquinolinone family of compounds, we observed an unexpected decarboxylation. The reaction of 4-nitrohomophthalic anhydride with a Schiff base formed on solid support leads to the formation of core structure. LC-MS and 1H NMR analysis confirmed the structure of unexpected intermediate. A library of 38,400 compounds was produced using this new synthetic approach.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1016205515959
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  • 6
    Electronic Resource
    Electronic Resource
    Library generation through successive substitution of trichlorotriazine (1996)
    Springer
    Molecular diversity 2 (1996), S. 75-80 
    Details
    ISSN: 1573-501X
    Keywords: Combinatorial library ; Small organic molecule ; Scaffold ; Solid-phase organic synthesis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary The decreasing reactivity of tri-, di- and monochlorotriazine was utilized for the solid-phase construction of a combinatorial library with three randomized positions, using 20 amino acids and 50 amines as building blocks. The first chlorine atom was selectively substituted by coupling a large excess of trichlorotriazine to the support-bound amino acid, thus avoiding simultaneous substitution of the second chlorine. The second and third diversity positions were selectively introduced by coupling amines at different temperatures. Mixtures of model compounds were synthesized and analyzed, showing the correct representation of all expected components. A library composed of 12 000 compounds was generated using this method.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01718703
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  • 7
    Electronic Resource
    Electronic Resource
    Bifunctional scaffolds as templates for synthetic combinatorial libraries (1996)
    Springer
    Molecular diversity 1 (1996), S. 177-182 
    Details
    ISSN: 1573-501X
    Keywords: Combinatorial chemistry ; Library ; Scaffold ; Solid-phase synthesis ; Streptavidin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary A small-molecule synthetic combinatorial library was designed and synthesized that features potential pharmacophores attached to a variety of small cyclic scaffolds. The synthesis of the library involved randomization of three types of building blocks: 20 amino acids, 10 aromatic hydroxy acids and 21 alcohols, totaling a library complexity of 4200 compounds. Mitsunobu polymer-supported etherification was used in the last randomization. The library compounds were attached to beads via an ester-bond linkage enabling both on-bead as well as in-solution screening. When the library was tested against a model target, streptavidin, specific binders were found. The structures of the most active compounds were determined from the fragmentation pattern in MS/MS experiments.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01544955
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  • 8
    Electronic Resource
    Electronic Resource
    High-volume cellular screening for anticancer agents with combinatorial chemical libraries: A new methodology (1996)
    Springer
    Molecular diversity 2 (1996), S. 57-63 
    Details
    ISSN: 1573-501X
    Keywords: Combinatorial chemical libraries ; Anticancer drugs ; Tumor cell line screening
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary A single-step cancer cell cytotoxic assay system for anticancer drug discovery has been developed which facilitates rapid screening of large combinatorial chemical libraries synthesized using the ‘one-bead-one-compound’ (OBOC) methodology. Each OBOC library bead incorporates two orthogonally cleavable linkers that release the bead-bound compound at a different pH. The assay utilizes high concentrations of tumor cells mixed directly with OBOC beads and plated in soft agarose containing tissue culture medium. One of the orthogonal linkers is cleaved at neutral pH in tissue culture releasing an aliquot of compound to diffuse at a relatively high local concentration into the soft agarose immediately surrounding the bead. Active compounds are identified visually from a clear ring of tumor cell lysis which forms within 48 h around just the rare bead releasing a cytotoxic compound. The bead releasing a cytotoxin is then plucked from the agar and the remaining compound still linked to the bead can be released for structural analysis, followed by compound resynthesis and confirmatory testing. This assay system has been successfully applied to identification of lead cytotoxic compounds from model peptidic and non-peptidic combinatorial chemical libraries. Use of this methodology may facilitate anticancer drug discovery.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01718701
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  • 9
    Electronic Resource
    Electronic Resource
    Molecular diversity comes of age ! (1995)
    Springer
    Molecular diversity 1 (1995), S. 1-3 
    Details
    ISSN: 1573-501X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01715803
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  • 10
    Electronic Resource
    Electronic Resource
    Solid-phase peptide synthesis by fragment condensation: Coupling in swelling volume (1999)
    Springer
    International journal of peptide research and therapeutics 6 (1999), S. 15-22 
    Details
    ISSN: 1573-3904
    Keywords: convergent peptide synthesis ; end-capping with 2,4-dinitrofluorobenzene ; protected peptide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary The condensation of short peptides to resin-bound fragments was examined with respect to high coupling yields with only a small molar excess of a peptide in the reaction solution. The best results were achieved by the addition of reactants (C-unprotected peptide, DIC, and HOBt) dissolved in a so-called swelling volume of an appropriate solvent to a dry resin with an attached N-deprotected peptide chain. Each coupling step was followed by the end-capping of unreacted resin-bound peptide with 2,4-dinitrofluorobenzene. The substituted dinitroaniline chromophore formed in this reaction made the detection and separation of deletion peptides easy. Both conventional and ‘swelling volume’ methods were compared on parallel syntheses of the HIV-1 protease C-terminal 78–99 fragment. The yields of the isolated heneicosapeptide were 21 and 81% in favor of the ‘swelling volume’ procedure.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02443614
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