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A class of medications known as antimetabolites prevents cells, especially cancer cells that divide quickly, from growing and developing normally. By effectively disguising themselves as the building units of DNA or RNA, they function by interfering with vital metabolic pathways. They can either prevent fresh DNA or RNA from being synthesized or they can introduce defective molecules into these essential structures, which can result in cell death. Among the antimetabolites most frequently utilized in the treatment of cancer is methotrexate. It functions as a folic acid analog, which is an essential chemical for the production of DNA. In order to bind to the enzyme dihydrofolate reductase, which is necessary for the synthesis of tetrahydrofolate, methotrexate and folic acid compete. Insufficient tetrahydrofolate prevents cells from synthesizing thymidine, which is a crucial building block of DNA. Because of this disturbance, the cell cycle is stopped, which stops cancer cells from growing. 5-fluorouracil (5-FU) is another well-known antimetabolite that is used to treat a variety of malignancies, including colorectal cancer. 5-FU is transformed into active metabolites that obstruct thymidine production. It prevents the thymidylate synthase enzyme from working, which is required to produce thymidine, a building block of DNA. 5-FU causes cell death by interfering with DNA synthesis and depriving the cell of thymidine. Cytarabine, sometimes referred to as Ara-C, is a medication used to treat lymphoma and leukemia. It is similar to the RNA and DNA building block cytidine. As soon as cytarabine enters the cell, it is transformed into its active form, cytarabine triphosphate, which contends with cytidine for DNA inclusion. Cytarabine triphosphate, on the other hand, prevents DNA polymerase from adding further nucleotides, which results in DNA chain termination and cell death. An antimetabolite called fludarabine is used to treat non-Hodgkin lymphoma and chronic lymphocytic leukemia (CLL). It is an analogue of purines that cells phosphorylate to create fludarabine triphosphate. By suppressing DNA polymerase and ribonucleotide reductase, two vital enzymes for DNA replication, this metabolite obstructs DNA synthesis. Antimetabolites affect both cancer cells and quickly dividing normal cells, which can result in a variety of side effects. These may include inhibition of the bone marrow, which can result in thrombocytopenia, leukopenia, and anemia. Moreover frequent are digestive disorders such nausea, vomiting, and diarrhea. Antimetabolites are still important weapons in the fight against cancer, nevertheless, and they give many patients hope despite these negative effects.