Molecular editing of NSC-666719 enabling discovery of benzodithiazinedioxide-guanidines as anticancer agents

Abstract

In this study, a unique strategy of scaffold-hopping-based molecular editing of a bioactive agent NSC-666719 was investigated, which led to the development of new benzodithiazinedioxide-guanidine based anticancer agents with Polβ inhibition.

Correction: A sequential Ugi–Smiles/transition-metal-free endo-dig Conia–ene cyclization: the selective synthesis of saccharin substituted 2,5-dihydropyrroles

One-pot synthesis of diaroyl benzothiepine-1,1-dioxides

Abstract

We report the one-pot two-step synthesis of diaroyl benzothiepine-1,1-dioxides via the rongalite-mediated double sulfination of α-bromoacetophenones followed by double condensation of the resulting 1,3-diaroyl sulfones and o-phthalaldehydes.

Synthesis of cis-fused cyclopentenone-pyrrolidine scaffolds via sequential aza-Piancatelli and Conia-ene type reactions in one pot

Abstract

A novel diastereoselective one-pot protocol has been developed through sequential execution of an aza-Piancatelli rearrangement and a Conia-ene type reaction under Lewis acid catalysis.

A gold(III)-catalyzed Conia-ene reaction for the direct synthesis of substituted pyrroles from β-ketopropargyl amines

Abstract

We disclose a gold-catalyzed conversion of unactivated β-ketopropargyl amines to polysubstituted pyrroles under mild, operationally simple conditions. This protocol was further extended to synthesize indolizine skeleton via a one-pot process.