A Concise Synthesis towards Antimalarial Quinazolinedione TCMDC-125133 and Its Anti-Proliferative Activity against MCF-7
Issued Date
2022-06-01
Resource Type
eISSN
14228599
DOI
Scopus ID
2-s2.0-85132874177
Journal Title
MolBank
Volume
2022
Issue
2
Rights Holder(s)
SCOPUS
Bibliographic Citation
MolBank Vol.2022 No.2 (2022)
Suggested Citation
Charoensutthivarakul S., Lohawittayanan D., Kanjanasirirat P., Jearawuttanakul K., Seemakhan S., Borwornpinyo S., Phanchana M. A Concise Synthesis towards Antimalarial Quinazolinedione TCMDC-125133 and Its Anti-Proliferative Activity against MCF-7. MolBank Vol.2022 No.2 (2022). doi:10.3390/M1358 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/83701
Title
A Concise Synthesis towards Antimalarial Quinazolinedione TCMDC-125133 and Its Anti-Proliferative Activity against MCF-7
Author's Affiliation
Other Contributor(s)
Abstract
Quinazolinedione 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.