Nuclear-substituted styryl ketone analogs: effects on neoplasms, microorganisms, and mitochondrial respiration of tumorous and normal cells.

Abstract	Analogs of some antineoplastic and cytotoxic Mannich bases derived from conjugated styryl ketones were prepared and evaluated for activity in the P-388 lymphocytic leukemia screen. Most of the new compounds had lower antineoplastic and murine toxicity than the parent compounds. Antimicrobial evaluation of some oximes and alcohols related to the Mannich bases revealed activity against certain Gram-positive bacteria and fungi. Primary pharmacological evaluation showed that some compounds containing a dimethylaminomethyl group displayed analgesic and antihistaminic properties. Five of the Mannich bases were evaluated as respiratory inhibitors in mitochondria derived from hepatic tumors, liver tissue from tumor-bearing animals, and normal rat liver. No statistical difference between the sensitivity of the three tissues to the compounds was obtained.
Authors	J R Dimmock, N W Hamon, L M Noble, D E Wright
Journal	Journal of pharmaceutical sciences (J Pharm Sci) Vol. 68 Issue 8 Pg. 1033-9 (Aug 1979) ISSN: 0022-3549 [Print] United States
PMID	314508 (Publication Type: Journal Article)
Chemical References	Amines Analgesics Anti-Inflammatory Agents, Non-Steroidal Antineoplastic Agents Histamine Antagonists Ketones Mannich Bases Styrenes
Topics	Amines (chemical synthesis) Analgesics Animals Anti-Inflammatory Agents, Non-Steroidal Antineoplastic Agents Chemical Phenomena Chemistry Drug Evaluation, Preclinical Histamine Antagonists (pharmacology) Ketones (chemical synthesis) Leukemia, Experimental (drug therapy, metabolism) Leukemia, Lymphoid (drug therapy, metabolism) Liver (metabolism) Liver Neoplasms, Experimental (metabolism) Mannich Bases (chemical synthesis, pharmacology, toxicity) Mice Microbial Sensitivity Tests Mitochondria (metabolism) Mitochondria, Liver (drug effects) Oxygen Consumption (drug effects) Rats Structure-Activity Relationship Styrenes (chemical synthesis)

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