Ellipticine derivatives with an affinity to the estrogen receptor. An approach to develop intercalating drugs with a specific effect on the hormone-dependent breast cancer

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Abstract
In order to obtain breast tumor directed agents, mixed compounds were prepared using estradiol or (E)-clomiphene as specific vectors for the breast tissue and a DNA intercalator from the ellipticine series as the cytotoxic agent. Among the newly synthesized ellipticine derivatives, only the 2-[3-aza-5-(3,17.beta.-dihydroxy-1,3,5-estratrien-17.alpha.-yl)-4-oxopentamethylene]ellipticinium bromide (24) shows the desired properties, DNA intercalation and affinity for estrogen receptor. Competition experiments with estradiol on the hormone-dependent human MCF-7 breast cancer cell line demonstrate that a transport by the estrogen receptor system is not involved in the antitumor activity of derivative 24.