Table 6 DNA Methyltransferares (DNMT) inhibitors in P. falciparum
From: Epigenetic regulation as a therapeutic target in the malaria parasite Plasmodium falciparum
Inhibitors | Structure | P. falciparum IC50 in µM | Specificity | Development stage | CC50 on mammalian cells in µM (Cell type) |
|---|---|---|---|---|---|
5-azacytidine |
| 1.5.103 [51] | Human DNMT [167] | FDA-approved in cancer therapy [167] | 2.3 (KG-1a acute myeloid leukemia)[168] |
Decitabine |
| 8.102 [51] | Human DNMT[167] | FDA-approved in cancer therapy [167] | 0.4 (KG-1a acute myeloid leukemia) [168] |
SGI-1027 |
| Human DNMT 1, 3A, 3B [169] | - | > 50 (H4IIE rat hepatoma) [169] | |
Quinoline-quinazoline derivative |
| 0.06 [132] | PfDNMT | Tested in standard chemosensitivity assays on ART-resistant strains | 2.5 (HepG2) [132] |
Quinazoline derivative |
| 0.019 [131] | PfDNMT3 | Tested in standard chemosensitivity assays on multidrug resistant strains | > 1 (Splenic) [131] |
