Acronycine is active against a broad spectrum of solid tumors. Structure activity relationships demonstrated the crucial role of the 1,2-double bond. A hypothesis of bioactivation into 1,2-epoxide led to the development of a series of 1,2- dihydroxy-1,2-dihydroacronycine and 1,2-dihydroxy-1,2-dihydrobenzo[b]acronycine diesters that exhibited an increased potency when compared with the parent compound.
Keywords: acronycine, solid tumors, increased potency, antitumor activity, murine leukemia cell line, cytotoxic activity, catalytic osmic oxidation, enlarged spectrum
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