Question

Discuss antimetabolites as anticancer agents

Answer 1

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Antimetabolite drugs were among the first effective chemotherapeutic agents discovered.  Classified as folic acid, pyrimidine or purine analogues, these compounds have similar chemical structures to molecules the body uses in nucleic acid (DNA and RNA) synthesis. Antimetabolites are similar to chemicals needed for normal biochemical activity, but differ enough that they interfere with normal cell function.

There are few clinically useful purine antagonists. Scientists conjecture that these purine antagonists stop synthesis by decreasing the production of the purine bases or that the antagonist molecules themselves may be incorporated into the DNA strands during synthesis and halt cell replication.  Without adequate amounts of the purine bases, nucleotide production stops and the cancer cell dies. Fludarabine or 2-fluoro-ara-amp is an antimetabolite of the purine class. It functions as a pro-drug. It is dephosphorylated to F-ara-ATP and enters the cancer cell.

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