Patamawadee SilalaiDumnoensun PruksakornArthit ChairoungduaKanoknetr SuksenRungnapha SaeengMahidol UniversityBurapha UniversityChiang Mai University2022-08-042022-08-042021-08-01Bioorganic and Medicinal Chemistry Letters. Vol.45, (2021)146434050960894X2-s2.0-85107125312https://repository.li.mahidol.ac.th/handle/123456789/76095Twenty six propargylamine mycophenolate analogues were designed and synthesized from mycophenolic acid 1 employing a key step A3-coupling reaction. Their cytotoxic activity was examined against six cancer cell lines. Compounds 6a, 6j, 6t, 6u, and 6z exhibited selective cytotoxicity towards neuroblastoma (SH-SY5Y) cancer cells and were less toxic to normal cells in comparison to the lead compound, MPA 1 and a standard drug, ellipticine. Molecular docking results suggested that compound 6a is fit well in the key amino acid of three proteins (CDK9, EGFR, and VEGFR-2) as targets in cancer therapy. The propargylamine mycophenolate scaffold might be a valuable starting point for development of new neuroblastoma anticancer drugs.Mahidol UniversityBiochemistry, Genetics and Molecular BiologyChemistryPharmacology, Toxicology and PharmaceuticsArticleSCOPUS10.1016/j.bmcl.2021.128135