Adisak ThanetchaiyakupSuparerk BorwornpinyoHassayaporn RattanaratPhongthon KanjanasiriratKedchin JearawuttanakulSawinee SeemakhanNutthawat ChuanopparatPaiboon NgernmeesriKasetsart UniversityMahidol University2022-08-042022-08-042021-10-12Tetrahedron Letters. Vol.82, (2021)18733581004040392-s2.0-85114674977https://repository.li.mahidol.ac.th/handle/20.500.14594/75996A simple and effective one-pot synthesis of substituted indolo[1,2-a]quinolines has been developed. The desired products were obtained in up to 98% yield when substituted 2-methyindoles were treated with 2-iodobenzaldehyde in the presence of Cs2CO3, CuI and L-proline. Our mechanistic study confirmed that the reaction sequence involved an intermolecular Knoevenagel reaction followed by an intramolecular Ullmann-type coupling reaction. Moreover, some of the synthesized compounds were found to be active against human breast (MCF-7) and colorectal (HCT-116) cancer cells with IC50 values of 27.96 μM and in the range of 6.21–46.91 μM, respectively.Mahidol UniversityBiochemistry, Genetics and Molecular BiologyChemistryPharmacology, Toxicology and PharmaceuticsArticleSCOPUS10.1016/j.tetlet.2021.153365