Antimetabolite

Floxuridine (FUDR) is an antimetabolite, floxuridine inhibits thymidylate synthase, resulting in disruption of DNA synthesis and cytotoxicity.

Gemcitabine (LY188011) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.

5-Fluorouracil (5-FU) is a uracil analog and inhibitor of DNA synthesis, exhibiting antitumor activity by affecting pyrimidine synthesis through thymidylate synthase inhibition; it induces apoptosis and autophagy.

Decitabine (Deoxycytidine) is a deoxycytidine analog, a DNA methyltransferase inhibitor with oral activity. Decitabine has antitumor activity and antimetabolic activity. Decitabine induces cell cycle arrest and apoptosis.

Fludarabine (Fludarabinum) is a fluorinated purine analog, an inhibitor of nucleic acid synthesis and an inhibitor of STAT1 activation. Fludarabine has antitumor activity and can be used for the treatment of leukemia and lymphoma.

1-Methylcytosine (4-amino-1-methylpyrimidin-2(1H)-one) is a methylated form of the cytosine and can be used as the nucleobase of hachimoji DNA paired with isoguanine.

MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC), with potential to treat tumor-induced bone disease (TIBD).

Peldesine (BCX 34) is an effective, competitive, reversible, and orally active inhibitor of purine nucleoside phosphorylase. Peldesine inhibits T-cell proliferation with an IC50 of 800 nM. Peldesine can be used in research on cutaneous T-cell lymphoma, psoriasis and HIV infection.

Ascamycin is a 5'-O-sulfonamide ribonucleoside antibiotic produced by Streptomyces spp. It exhibits selective antibacterial activity against Xanthomonas species, inhibiting Xanthomonas citri, Xanthomonas oryzae, and phage with MIC values of 0.4 μg mL, 12.5 μg mL, and 12.5 μg mL respectively.

Rabacfosadine (GS-9219) is a novel dual pre-drug of the acyclic nucleotide phosphonate PMEG to tumor lymphocytes for the study of lymphoma.

Netivudine is a potent nucleoside reverse transcriptase inhibitor (NRTIs), a nucleoside analogue with anti-varicella zoster virus activity that can be used to treat human immunodeficiency virus (HIV) infection. Netivudine works by inhibiting reverse transcriptase, which reduces viral load in the body and slows the progression of the disease through its inhibitory effect.

6-Mercaptopurine (6-MP) is an antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.

Bendamustine hydrochloride (EP-3101) (IC50 of 50 μM) is an alkylating agent associated with DNA damage.

Clofarabine (Clofarex)m, a second generation purine nucleoside analog with antineoplastic activity, inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.

5,6-Dihydro-5-methyluracil (Dihydrothymine) is an intermediate breakdown product of thymine.

Ganciclovir (2'-Nor-2'-deoxyguanosine) is an ACYCLOVIR analog that is a potent inhibitor of the Herpesvirus family including cytomegalovirus. Ganciclovir is used to treat complications from AIDS-associated cytomegalovirus infections.

Orotic acid (Vitamin B13) is an intermediate product in pyrimidine metabolism.

Adenosine (D-Adenosine) is a natural product, a ribonucleoside consisting of adenine bound to ribose. Adenosine has vasodilatory, antiarrhythmic and analgesic effects.

Dacarbazine (DTIC-Dome) is an antineoplastic agent. It has significant activity against melanomas.

Cytarabine (Ara-C) is a nucleoside analog, an inhibitor of DNA synthesis (IC50=16 nM). Cytarabine inhibits DNA polymerase and induces cell cycle arrest, autophagy, and apoptosis. Cytarabine has antitumor activity.

5-Azacytidine (Ladakamycin) is a cytidine nucleoside analog, a DNA methylation inhibitor with specificity. 5-Azacytidine regulates gene expression by decreasing the level of DNA methylation. 5-Azacytidine induces autophagy and has antitumor activity.

Tegafur (FT 207) is a congener of the antimetabolite fluorouracil with antineoplastic activity. Tegafur is a prodrug that is gradually converted to fluorouracil in the liver by the cytochrome P-450 enzyme.

Stavudine (BMY-27857), a nucleoside reverse transcriptase inhibitor analog of thymidine, has activity against HIV.

Capecitabine (Capecitibine) is a fluoropyrimidine carbamate belonging to the class of antineoplastic agents called antimetabolites. As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil (5-FU); subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate for incorporation into the RNA strand.