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 of biological activities including antimalarial, anticancer, anti-inflammatory, and others. TCMDC-125133, whose structure features a quinazolinedione core, exhibits promising antimalarial activity...
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MDPI AG
2022-04-01
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| Series: | Molbank |
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| Online Access: | https://www.mdpi.com/1422-8599/2022/2/M1358 |
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| author | Sitthivut Charoensutthivarakul Duangporn Lohawittayanan Phongthon Kanjanasirirat Kedchin Jearawuttanakul Sawinee Seemakhan Suparerk Borwornpinyo Matthew Phanchana |
| author_facet | Sitthivut Charoensutthivarakul Duangporn Lohawittayanan Phongthon Kanjanasirirat Kedchin Jearawuttanakul Sawinee Seemakhan Suparerk Borwornpinyo Matthew Phanchana |
| author_sort | Sitthivut Charoensutthivarakul |
| collection | DOAJ |
| description | 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 <i>P. falciparum</i> 3D7 and antiproliferative activity against MCF-7 cell line. |
| first_indexed | 2024-03-09T22:56:57Z |
| format | Article |
| id | doaj.art-3f85c6565d944e4099ec06dd4cf4a0e8 |
| institution | Directory Open Access Journal |
| issn | 1422-8599 |
| language | English |
| last_indexed | 2024-03-09T22:56:57Z |
| publishDate | 2022-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molbank |
| spelling | doaj.art-3f85c6565d944e4099ec06dd4cf4a0e82023-11-23T18:08:11ZengMDPI AGMolbank1422-85992022-04-0120222M135810.3390/M1358A Concise Synthesis towards Antimalarial Quinazolinedione TCMDC-125133 and Its Anti-Proliferative Activity against MCF-7Sitthivut Charoensutthivarakul0Duangporn Lohawittayanan1Phongthon Kanjanasirirat2Kedchin Jearawuttanakul3Sawinee Seemakhan4Suparerk Borwornpinyo5Matthew Phanchana6Innovative Molecular Discovery Laboratory (iMoD), School of Bioinnovation and Bio-Based Product Intelligence, Faculty of Science, Mahidol University, Bangkok 10400, ThailandInnovative Molecular Discovery Laboratory (iMoD), School of Bioinnovation and Bio-Based Product Intelligence, Faculty of Science, Mahidol University, Bangkok 10400, ThailandExcellent Center for Drug Discovery (ECDD), Faculty of Science, Mahidol University, Bangkok 10400, ThailandExcellent Center for Drug Discovery (ECDD), Faculty of Science, Mahidol University, Bangkok 10400, ThailandExcellent Center for Drug Discovery (ECDD), Faculty of Science, Mahidol University, Bangkok 10400, ThailandExcellent Center for Drug Discovery (ECDD), Faculty of Science, Mahidol University, Bangkok 10400, ThailandDepartment of Molecular Tropical Medicine and Genetics, Faculty of Tropical Medicine, Mahidol University, Bangkok 10400, ThailandQuinazolinedione 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 <i>P. falciparum</i> 3D7 and antiproliferative activity against MCF-7 cell line.https://www.mdpi.com/1422-8599/2022/2/M1358quinazolinedione derivativesantimalarial activityantiproliferative activity |
| spellingShingle | Sitthivut Charoensutthivarakul Duangporn Lohawittayanan Phongthon Kanjanasirirat Kedchin Jearawuttanakul Sawinee Seemakhan Suparerk Borwornpinyo Matthew Phanchana A Concise Synthesis towards Antimalarial Quinazolinedione TCMDC-125133 and Its Anti-Proliferative Activity against MCF-7 Molbank quinazolinedione derivatives antimalarial activity antiproliferative activity |
| title | A Concise Synthesis towards Antimalarial Quinazolinedione TCMDC-125133 and Its Anti-Proliferative Activity against MCF-7 |
| title_full | A Concise Synthesis towards Antimalarial Quinazolinedione TCMDC-125133 and Its Anti-Proliferative Activity against MCF-7 |
| title_fullStr | A Concise Synthesis towards Antimalarial Quinazolinedione TCMDC-125133 and Its Anti-Proliferative Activity against MCF-7 |
| title_full_unstemmed | A Concise Synthesis towards Antimalarial Quinazolinedione TCMDC-125133 and Its Anti-Proliferative Activity against MCF-7 |
| title_short | A Concise Synthesis towards Antimalarial Quinazolinedione TCMDC-125133 and Its Anti-Proliferative Activity against MCF-7 |
| title_sort | concise synthesis towards antimalarial quinazolinedione tcmdc 125133 and its anti proliferative activity against mcf 7 |
| topic | quinazolinedione derivatives antimalarial activity antiproliferative activity |
| url | https://www.mdpi.com/1422-8599/2022/2/M1358 |
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