Antitumor agents. II. Bis(guanylhydrazones) of anthracene-9,10-dicarboxaldehydes

Autor:	Patrick T. Izzo, J. D. Warren, Roslyn E. Wallace, Frederick E. Durr, S. A. Lang, Keith Chadwick Murdock, Paul F. Fabio, Ralph Grassing Child, Robert B. Angier, R. V. Citarella, Y. Lin, Ving J. Lee
Rok vydání:	1982
Předmět:	chemistry.chemical_classification Melanoma Hydrazone Half-life Plasma cell medicine.disease chemistry.chemical_compound Leukemia medicine.anatomical_structure chemistry Drug Discovery medicine Cancer research Molecular Medicine Bisantrene Sarcoma DNA
Zdroj:	Journal of Medicinal Chemistry. 25:505-518
ISSN:	1520-4804 0022-2623
DOI:	10.1021/jm00347a006
Popis:	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.
Databáze:	OpenAIRE
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