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Abstract
Five cytotoxic Mannich bases (5-dimethylamino-1-substituted phenyl- 1-penten-3-ones), three having antineoplastic activity, were evaluat,ed for respiratory-inhibiting properties in rat liver mitochondria in the presence of lour substrates: succinate, glutamate, 3-hydroxybutyrate, and palmitylcarnitine. Four compounds (Ib-Ie) showed significant inhibiting properties which, on occasion, were reversed partially by coenzyme Q10. Evaluation of the spectra of the mitochondria1 cytochromes indicated that Ib-Ie blocked the electron transport chain prior to the sequence of cytochromes. Since inhibition occurred when different substrates were used, a common site of action for Ib-Ie is likely; competition of lb-lc with coenzyme Q10 probably occurs. Compounds Ia-Ie inhibited RNA polymerase from Swiss muuse kidney cells but were virtually bereft of activity versus RNA polymerase from L-1210 leukemia cells. Polarography of the Mannich bases and the related styryl ketones showed that antineoplastic activity was associated with higher half-wave potentials.
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