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Antitumor agents. II. Bis(guanylhydrazones) of anthracene-9,10-dicarboxaldehydes
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1982
Year
Tumor BiologyMedicinal ChemistryRing-substituted Anthracene-9,10-dicarboxaldehyde IntermediatesAntitumor AgentsMedicineStructure-activity RelationshipsTumor TargetingAnti-cancer AgentColon Tumor 26Heterocycle ChemistryCancer TreatmentPharmacologyRadiation OncologyPharmaceutical ChemistryCancer ResearchDrug Discovery
9,10-Anthracenedicarboxaldehyde bis[(4,5-dihydro-1H-imidazol-2-yl)hydrazone] (bisantrene, VI-1) showed anticancer activity in mice vs. both leukemias and solid tumors. Increases in life span vs. the following neoplasms were: P-388 leukemia, 137%; B-16 melanoma, 122%; Lieberman plasma cell tumor, greater than 85%; colon tumor 26, 150%; Ridgway osteogenic sarcoma, 85%. There were significant numbers of long-term survivors. Both DNA and RNA synthesis were strongly inhibited. The drug was resistant to biodegradation and was bound strongly to tissues; in monkeys the half-life for disappearance from serum was 6 days. Related hydrazones were synthesized, and structure-activity relationships are discussed. Two routes to ring-substituted anthracene-9,10-dicarboxaldehyde intermediates were developed.