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Topic 5 Nucleic Acids as Drug Targets

Topic 5 Nucleic Acids as Drug Targets

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3. DRUGS ACTING ON DNA<br />

3.2 Alkylating agents<br />

Mechlorethamine analogues<br />

Aromatic ring - e withdrawing effect<br />

N is less nucleophilic<br />

Less reactive alkylating agent<br />

Selective for stronger nucleophiles<br />

(e.g. guanine)<br />

N<br />

Cl<br />

Cl<br />

O<br />

HN<br />

O<br />

N<br />

H<br />

Uracil mustard<br />

Used vs leukemia<br />

Attached to a nucleic acid building<br />

block<br />

Concentrated in f<strong>as</strong>t growing cells<br />

(tumours)<br />

Some selectivity<br />

N<br />

Cl<br />

Cl

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