Experimental procedures, progress of the substrate conversion for heterocyclization reaction (Tables S1 and S2, Figure S18) and monitoring of the reaction mechanism (Figures S19−S22); biological data (Table S4) and assays details, copy of 1 H, 13 C NMR, FT-IR and ESI MS spectra (Figures S23−S88) and spectral assignments, X-ray structural details of 1a−11a (Figures S1−S17; Table S3). (PDF)Accession Codes CCDC 2155685−2155694 and 2245620 contain the supplementary crystallographic data for this paper. These data can be obtained free of charge via www.ccdc.cam.ac.uk