期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 12, 期 39, 页码 7659-7672出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c4ob00835a
关键词
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资金
- National Institutes of Health [GM 86192, GM 24539]
- Robert A. Welch Foundation [F-0652]
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.
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