1,4-disubstituted anthracene antitumor agents

Bhashyam S. Iyengar, Robert T. Dorr, David S. Alberts, Anikó M. Sólyom, Mary Krutzsch, William A. Remers

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25 Scopus citations


Three different types of 1,4-disubstituted anthracenes were synthesized, and their cytotoxicity in a panel of tumor cells was compared with that of the corresponding 9,10-disubstituted anthracenes. The panel contained human myeloma, melanoma, colon, and lung cancer cells and sensitive and multidrug- resistant murine L1210 leukemia cells. These compounds had [[(dimethylamino)ethyl]amino]methyl, N-[(dimethylamino)ethyl]carbamoyl, and carboxaldehyde (4,5-dihydro-1H-imidazol-2-yl)hydrazone side chains. The 1,4- diamide was more potent across the tumor panel than the corresponding 9,10- isomer, but the 1,4-diamine and the 1,4-hydrazone were less potent than their 9,10-isomers. Although the 1,4-hydrazone was active against P388 leukemia in mice, it was inactive against L1210 leukemia. Within each pair of compounds, the one with greater average potency against tumor cells gave a greater increase in the transition melt temperature of DNA.

Original languageEnglish (US)
Pages (from-to)3734-3738
Number of pages5
JournalJournal of Medicinal Chemistry
Issue number23
StatePublished - Nov 20 1997

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    Iyengar, B. S., Dorr, R. T., Alberts, D. S., Sólyom, A. M., Krutzsch, M., & Remers, W. A. (1997). 1,4-disubstituted anthracene antitumor agents. Journal of Medicinal Chemistry, 40(23), 3734-3738. https://doi.org/10.1021/jm970308+