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Communication

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

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Innovative Molecular Discovery Laboratory (iMoD), School of Bioinnovation and Bio-Based Product Intelligence, Faculty of Science, Mahidol University, Bangkok 10400, Thailand
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Excellent Center for Drug Discovery (ECDD), Faculty of Science, Mahidol University, Bangkok 10400, Thailand
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Center for Neuroscience, Faculty of Science, Mahidol University, Bangkok 10400, Thailand
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Department of Biotechnology, Faculty of Science, Mahidol University, Bangkok 10400, Thailand
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Department of Molecular Tropical Medicine and Genetics, Faculty of Tropical Medicine, Mahidol University, Bangkok 10400, Thailand
*
Author to whom correspondence should be addressed.
Academic Editor: Stanislav Kafka
Molbank 2022, 2022(2), M1358; https://doi.org/10.3390/M1358
Received: 25 February 2022 / Revised: 13 April 2022 / Accepted: 18 April 2022 / Published: 21 April 2022
(This article belongs to the Special Issue Quinoline, Derivatives and Applications)
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. View Full-Text
Keywords: quinazolinedione derivatives; antimalarial activity; antiproliferative activity quinazolinedione derivatives; antimalarial activity; antiproliferative activity
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MDPI and ACS Style

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 2022, 2022, M1358. https://doi.org/10.3390/M1358

AMA Style

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. 2022; 2022(2):M1358. https://doi.org/10.3390/M1358

Chicago/Turabian Style

Charoensutthivarakul, Sitthivut, Duangporn Lohawittayanan, Phongthon Kanjanasirirat, Kedchin Jearawuttanakul, Sawinee Seemakhan, Suparerk Borwornpinyo, and Matthew Phanchana. 2022. "A Concise Synthesis towards Antimalarial Quinazolinedione TCMDC-125133 and Its Anti-Proliferative Activity against MCF-7" Molbank 2022, no. 2: M1358. https://doi.org/10.3390/M1358

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