Abstract
The preparation and examination of 3 and 4 and their unnatural epimers 6 and 7 by following a new and alternative synthesis of 2 was conducted to assess the role of the pyrimidine C4 amine of bleomycin A2 (1) and deglycobleomycin A2 (2). The agent 3 bearing a pyrimidine C4 dimethylamino substituent exhibited a substantially diminished DNA cleavage efficiency (10−15×) relative to 2 and the loss of the characteristic 5‘-GC/5‘-GT cleavage selectivity. The agent 4 in which the pyrimidine C4 amino group was removed exhibited an even greater diminished DNA cleavage efficiency (30×) relative to that for 2. For this agent, the characteristic cleavage selectivity is either slightly or significantly reduced depending on the assay conditions. Even in the instances where it was not substantially altered, the ability to detect it required a temperature of 4 versus 25−37 °C. This information and temperature dependence suggest a reduced binding interaction and are consistent with the participation of the pyrimidine C4 a...
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