Charoensutthivarakul S.Lohawittayanan D.Kanjanasirirat P.Jearawuttanakul K.Seemakhan S.Borwornpinyo S.Phanchana M.Mahidol University2023-06-182023-06-182022-06-01MolBank Vol.2022 No.2 (2022)https://repository.li.mahidol.ac.th/handle/20.500.14594/83701Quinazolinedione is one of the most notable pharmacophores in drug discovery due to its broad spectrum of biological activities including antimalarial, anticancer, anti-inflammatory, and others. TCMDC-125133, whose structure features a quinazolinedione core, exhibits promising antimalarial activity and low toxicity as described in the GlaxoSmithKline (GSK) report. Herein, a concise four-step synthesis towards quinazolinedione TCMDC-125133 is described using low cost goods and greener alternatives where possible. All synthesized compounds were characterized using polarimetry, IR, NMR, and mass spectrometry. The in-house synthesized TCMDC-125133 was evaluated for its antimalarial activity against P. falciparum 3D7 and antiproliferative activity against MCF-7 cell line.Biochemistry, Genetics and Molecular BiologyNoteSCOPUS10.3390/M13582-s2.0-8513287417714228599