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An efficient synthesis of simplified azinomycin A and B analogues 1 and 2 (see picture) is described, and it is demonstrated that only 1, bearing both the epoxide and aziridine, induces interstrand cross-links in double-stranded DNA. Remarkably, a compound structurally related to 1 but devoid of the aziridine ring exhibited comparable in vitro cytotoxicity, suggesting that in cells the epoxide is largely responsible for the antitumor activity of these agents.
Hartley et al. (2000) studied this question.