2. Academic Validation
  3. Formation of squaric acid amides of anthracycline antibiotics. Synthesis and cytotoxic properties

Formation of squaric acid amides of anthracycline antibiotics. Synthesis and cytotoxic properties

  • Bioorg Med Chem Lett. 2004 Sep 20;14(18):4783-9. doi: 10.1016/j.bmcl.2004.06.072.
Anna Tevyashova 1,  Ferenc Sztaricskai,  Gyula Batta,  Pál Herczegh,  András Jeney
Affiliations

Affiliation

  • 1 Research Group for Antibiotics of the Hungarian Academy of Sciences, and Department of Pharmaceutical Chemistry, University of Debrecen, Debrecen, PO Box 70, H-4010 Hungary.
PMID: 15324908 DOI: 10.1016/j.bmcl.2004.06.072
Abstract

The reaction of the anthracycline glycoside Antibiotics 1-3 with the squaric acid ester 4 gave the squaric acid amide esters 5-7 under neutral conditions, whereas over pH7 the products are the symmetric diamides (8, 9, 11, and 12). Of the prepared compounds 11 was the most active on MCF-7 human mammary adenocarcinoma cells.

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