title: Evolution of a strategy for preparing bioactive small molecules by sequential multicomponent assembly processes, cyclizations, and diversification.
abstract: A strategy for generating diverse collections of small molecules has been developed that features a multicomponent assembly process (MCAP) to efficiently construct a variety of intermediates possessing an aryl aminomethyl subunit. These key compounds are then transformed via selective ring-forming reactions into heterocyclic scaffolds, each of which possesses suitable functional handles for further derivatizations and palladium-catalyzed cross coupling reactions. The modular nature of this approach enables the facile construction of libraries of polycyclic compounds bearing a broad range of substituents and substitution patterns for biological evaluation. Screening of several compound libraries thus produced has revealed a large subset of compounds that exhibit a broad spectrum of medicinally-relevant activities.
authors.affiliation: Department of Chemistry, The University of Texas at Austin, 1 University Station A5300, Austin, TX 78712-0165, USA. sfmartin@mail.utexas.edu.
authors.forename: James J
authors.initials: JJ
authors.lastname: Sahn
authors.forename: Brett A
authors.initials: BA
authors.lastname: Granger
authors.forename: Stephen F
authors.initials: SF
authors.lastname: Martin
mesh_terms: D002384:Catalysis; D003500:Cyclization; D006801:Humans; D009930:Organic Chemicals / Q000737:chemistry*; D054852:Small Molecule Libraries / Q000737:chemistry*
chemical_list: D009930:Organic Chemicals; D054852:Small Molecule Libraries