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...
Saved in:
| Main Author: | |
|---|---|
| Other Authors: | |
| Format: | Note |
| Published: |
2023
|
| Subjects: | |
| Online Access: | https://repository.li.mahidol.ac.th/handle/123456789/83701 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| Institution: | Mahidol University |
| Summary: | 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. |
|---|