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

Autor:	Charoensutthivarakul, Sitthivut, Lohawittayanan, Duangporn, Kanjanasirirat, Phongthon, Jearawuttanakul, Kedchin, Seemakhan, Sawinee, Borwornpinyo, Suparerk, Phanchana, Matthew
Předmět:	MASS spectrometry CHEMICAL synthesis DRUG discovery CELL lines POLARIMETRY
Zdroj:	Molbank; Jun2022, Vol. 2022 Issue 2, pM1358-N.PAG, 9p
Abstrakt:	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. [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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