Table 1.
Drugs targeting DHFR (status and structure of drugs targeting DHFR)
| Drugs | Status | Diseases | |
|---|---|---|---|
| Pyrimethamine | Approved | Antimalarial |
|
| Cycloguanil | Approved | Antimalarial |
|
| Methotrexate | Approved | Leukemias, choriocarcinoma, different cancers |
|
| Trimetrexate | Approved |
Pneumocystis pneumonia Antineoplastic and antiviral activity |
|
| Pentamidine | Approved | African trypanosomiasis |
|
| Pemetrexed | Approved | Chemotherapeutic agent |
|
| Sulfadoxine | Approved | Antimalarial (Sulfadoxine targets Plasmodium dihydropteroate synthase and dihydrofolate reductase) |
|
| Chlorproguanil | Approved | Prophylactic plasmodium |
|
| Proguanil | Approved | Malaria |
|
| Urea | Approved | Keratolytic |
|
| Pralatrexate | Approved | Chemotherapeutic agent |
|
| Lamotrigine | Approved | Antiepileptic drug |
|
| Trimethoprim | Approved | Antibiotic for bacterial infections |
|
| Gentamicin | Approved | Antibiotic for bacterial infections |
|
| Folic acid | Approved | Certain types of anemia |
|
| Aminopterin | Withdrawn |
|
|
| P218 | Under investigation | Antimalarial |
|
| Brodimoprim-4,6-Dicarboxylate | Under investigation | Investigational |
|
| 2,4-Diamino-5-(3,4,5-Trimethoxy-Benzyl)-Pyrimidin-1-Ium | Under investigation | Investigational |
|
| 7-[2-Methoxy-1-(methoxymethyl)ethyl]-7 h-pyrrolo[3,2-f] quinazoline-1,3-diamine | Under investigation | Investigational |
|
| 7-(1-Ethyl-Propyl)-7 h-Pyrrolo-[3,2-F]Quinazoline-1,3-Diamine | Under investigation | Investigational |
|
| 5-Phenylsulfanyl-2,4-Quinazolinediamine | Under investigation | Investigational |
|
| 5-Chloryl-2,4,6-Quinazolinetriamine | Under investigation | Investigational |
|
| 5-[4-Tert-Butylphenylsulfanyl]-2,4-Quinazolinediamine | Under investigation | Investigational |
|
| 5-[(4-Methylphenyl)Sulfanyl]-2,4-Quinazolinediamine | Under investigation | Investigational |
|
| 5-(4-Morpholin-4-Yl-Phenylsulfanyl)-2,4-Quinazolinediamine | Under investigation | Investigational |
|
| 5-(4-Methoxyphenoxy)-2,4-Quinazolinediamine | Under investigation | Investigational |
|
| 2,4-Diamino-5-Methyl-6-[(3,4,5-Trimethoxy-N-Methylanilino)Methyl]Pyrido[2,3-D]Pyrimidine | Under investigation | Investigational |
|
| 6-(Octahydro-1 h-Indol-1-Ylmethyl)Decahydroquinazoline-2,4-Diamine | Under investigation | Investigational |
|
| N6-(2,5-Dimethoxy-Benzyl)-N6-Methyl-Pyrido[2,3-D]Pyrimidine-2,4,6-Triamine | Under investigation | Investigational |
|
| 2,4-Diamino-6-[N-(3',4',5'-Trimethoxybenzyl)-N-Methylamino]Pyrido[2,3-D]Pyrimidine | Under investigation | Investigational |
|
| Sri-9662 | Under investigation | Antifolate |
|
| Epigallocatechin gallate | Under investigation | Flavonoid |
|
| (S)-iclaprim | Under investigation | In vitro activity against Gram-positive bacteria |
|
| 5-[3-(2,5-dimethoxyphenyl)prop-1-yn-1-yl]-6-ethylpyrimidine-2,4-diamine | Under investigation | Investigational |
|
| 5-[[(2R)-2-cyclopropyl-7,8-dimethoxy-2H-chromen-5-yl]methyl]pyrimidine-2,4-diamine | Under investigation | Investigational | |
| Biopterin | Under investigation | Endogenous enzyme cofactors |
|
| 5-[(3R)-3-(5-methoxybiphenyl-3-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine | Under investigation | Investigational |
|
| 5-[(3R)-3-(5-methoxy-4'-methylbiphenyl-3-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine | Under investigation | Investigational |
|
| 5-[(3R)-3-(5-methoxy-3',5'-dimethylbiphenyl-3-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine | Under investigation | Investigational |
|
| 5-[(3R)-3-(5-methoxy-2',6'-dimethylbiphenyl-3-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine | Under investigation | Investigational |
|
| 2,4-Diamino-6-[N-(2',5'-Dimethoxybenzyl)-N-Methylamino]Quinazoline | Under investigation | Investigational |
|
| 2,4-Diamino-6-[N-(3',5'-Dimethoxybenzyl)-N-Methylamino]Pyrido[2,3-D]Pyrimidine | Under investigation | Investigational |
|
| 5-[3-(2,5-dimethoxyphenyl)prop-1-yn-1-yl]-6-ethylpyrimidine-2,4-diamine | Under investigation | Investigational | |
| [N-(2,4-Diaminopteridin-6-YL)-methyl]-dibenz[B,F]azepine | Under investigation | Investigational |
|
| (4aS)-5-[(2,4-diaminopteridin-6-yl)methyl]-4a,5-dihydro-2H-dibenzo[b,f]azepin-8-ol | Under investigation | Investigational |
|
| (2R,6S)-6-{[methyl(3,4,5-trimethoxyphenyl)amino]methyl}-1,2,5,6,7,8-hexahydroquinazoline-2,4-diamine | Under investigation | Investigational |
|