Principles of Chemotherapy - Experimental Oncology Graduate Study
Principles of Chemotherapy - Experimental Oncology Graduate Study
Principles of Chemotherapy - Experimental Oncology Graduate Study
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1. Alkylating agents• Highly reactive electrophilic drugs that form covalent bonds with anumber <strong>of</strong> electron-rich groups <strong>of</strong> biological molecules (such as amino,phosphate, sulfhydryl, and hydroxyl groups).• Have either 1 (mon<strong>of</strong>unctional) or 2 (bifunctional) electrophilic sidechains.• Major mechanism <strong>of</strong> cytotoxicity involves interaction with DNA bases.• Bifunctional drugs can form DNA interstrand cross-links (ISCs).• Major classes <strong>of</strong> alkylating agents include:(a) nitrogen mustards (e.g., melphalan, cyclophosphamide);(b) chloroethyl nitrosoureas (e.g., BCNU, CCNU, methyl-CCNU); and(c) methane sulfonic acid esters (e.g., busulfan).10
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