Synlett · 2018 · 28 citations · 7 references
PharmacyMedicinal ChemistryOncologyCancer PharmacologyDrug DiscoverySynthetic Medicinal ChemistryMacrocycle SynthesisNatural Product Drug DiscoveryAntiproliferative AgentsAntiproliferative Drug ActionBenzothiazole SynthesisChalcogenide SynthesisFunctional Group ToleranceOne-pot Heterocycle Synthesis
An efficient and convenient copper-catalyzed oxidative chalcogenation of benzothiazoles and imidazo[1,2-a]pyridines with sulfur/selenium powder and aryl boronic acids was developed. This procedure allows access to a wide range of structurally diverse arylchalcogen-substituted benzothiazoles/imidazo[1,2-a]pyridines in good yields and with good functional group tolerance. A biological evaluation revealed that some of the obtained products exhibited in vitro antiproliferative activities on human-derived lung, stomach, esophageal, and breast cancer cell lines.
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