A Concise Synthesis towards Antimalarial Quinazolinedione TCMDC-125133 and Its Anti-Proliferative Activity against MCF-7

Quinazolinedione is one of the most notable pharmacophores in drug discovery due to its broad spectrum biological activities including antimalarial, anticancer, anti-inflammatory, and others. TCMDC-125133, whose structure features a quinazolinedione core, exhibits promising antimalarial activity low toxicity as described GlaxoSmithKline (GSK) report. Herein, concise four-step synthesis towards TCMDC-125133 using cost goods greener alternatives where possible. All synthesized compounds were characterized polarimetry, IR, NMR, mass spectrometry. The in-house was evaluated for against P. falciparum 3D7 antiproliferative MCF-7 cell line.