Ch3

Ecteinascidin-743 (trabectedin)

Recognition of the saframycins by the DNA minor groove shows some specificity towards 5'-GGG and 5'-GGC sequences,47 and is followed by alkylation. Saframycin S, one of the most active saframycins, is active in the quinone form, which has been explained through the formation of iminium cation 6.26 and subsequent covalent binding to DNA involving attack by guanine amino groups to give aminal 6.27 48 (Fig. 6.13).

In the case of saframycin S, there is a second type of covalent binding mechanism involving previous reduction to dihydroquinone, which facilitates the formation of the alkylating iminium species.49 The less-reactive saframycin A only alkylates DNA in its hydroquinone form,50 and indeed several hydroquinone analogues of saframycin A have been shown to be up to 20-fold more active than the parent

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