pyrimidine purine antineoplastics Flashcards
Leflunomide
disrupts carbomyl phosphate –> orotic acid step in purine synthesis
Hydroxyurea
disrupts UDP –> dUDP step in purine synthesis via ribonucleotide reductase inhibition
5-FU
disrupts the dUMP–> dTMP via THF(methylene)–> DHF step via inhibition of thymidylate synthesis
MTX
disrupts DHF –> THF via dihydrofolate reductase
TMP
disrupts DHF –> THF via dihydrofolate reductase
pyrimethamine
disrupts DHF –> THF via dihydrofolate reductase
6-MP
disrupts PRPP–>IMP
Mycophenolate, ribarvirin
disrupts IMP–> GMP
Pyrimidine synthesis disrupters
Leflunomide, MTX, TMP, pyrimethamine, 5-FU
Purine synthesis disrupters
6-MP
mycophenolate, ribavirin
inhibits dihydroorotate dehydrogenase
leflunomide
inhibits dihydrofolate reductase in humans, bacteria, and protozoa respectively
- MTX - humans
- TMP - bacteria
- pyrimethamine - protozoa
prodrug is azathioprine
6-mercaptopurine, inhibits de novo purine synthesis
inhibit inosine monophosphate dehydrogenase
mycophenolate and ribovirin
inhibits ribonucleotide reductase
hydroxyurea