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Many chemotherapeutic agents are available for the management of malignant diseases. However, numerous of these agents require activation before they can express anticancer activities. Several types of activation are reviewed, including reductive, oxidative, thiol addition (nucleophile), metal complexation, and photochemical processes. An ideal cancer chemotherapeutic prodrug is completely inactive until activated by a specific process and may be used to elicit specific cancer cell kill whilst leaving normal tissues unharmed. The understanding of the mechanism of activation is important for the design of prod rug that is completely inactive until activated by one of the process mention above.

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