Benzimidazole-based analogues of cis- and trans-Epo A, 2 and 3, have been prepared through stereoselective total synthesis. Both compounds are highly potent antiproliferative agents, but the effects of side-chain replacement on cellular activity are ambivalent. While significantly enhanced potency is observed against a drug-sensitive human cancer cell line, 2 and 3 more susceptible to P-gp-mediated drug efflux than Epo A or trans-Epo A.
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Cachoux et al. (2005) studied this question.
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