2. Academic Validation
  3. Dehydroabietylamine-substituted trifluorobenzene sulfonamide rhodamine B hybrids as anticancer agents overcoming drug resistance

Dehydroabietylamine-substituted trifluorobenzene sulfonamide rhodamine B hybrids as anticancer agents overcoming drug resistance

  • Eur J Med Chem. 2024 Jul 10:276:116667. doi: 10.1016/j.ejmech.2024.116667.
Niels V Heise 1,  Sven J Meyer 1,  René Csuk 2,  Thomas Mueller 3
Affiliations

Affiliations

  • 1 Organic Chemistry, Martin-Luther University Halle-Wittenberg, Kurt-Mothes-Str. 2, D-06120, Halle (Saale), Germany.
  • 2 Organic Chemistry, Martin-Luther University Halle-Wittenberg, Kurt-Mothes-Str. 2, D-06120, Halle (Saale), Germany. Electronic address: rene.csuk@chemie.uni-halle.de.
  • 3 University Clinic for Internal Medicine IV, Hematology/Oncology, Medical Faculty, Martin-Luther-University Halle-Wittenberg, Ernst-Grube-Str. 40, D-06120, Halle (Saale), Germany.
PMID: 38996651 DOI: 10.1016/j.ejmech.2024.116667
Abstract

Attachment of a conjugate assembled from a novel fluorinated Carbonic Anhydrase Inhibitor and rhodamine B onto dehydroabietylamine (DHA) or cyclododecylamine led to first-in-class conjugates of good cytotoxicity; thereby IC50 values (from SRB assays; employed tumor cell lines A2780, A2780Cis, A549, HT29, MCF7, and non-malignant human fibroblasts CCD18Co) between 0.2 and 0.7 μM were found. Both conjugates showed similar cytotoxic activity but the dehydroabietylamine derived conjugate outperformed its cyclododecyl analog in terms of tumor cell/non-tumor cell selectivity. Both conjugates accumulate intracellular, and the DHA conjugate was able to overcome drug resistance which is effective independent of the expression status of Carbonic Anhydrase IX.

Keywords

Conjugates; Cytotoxicity; Dehydroabietylamine.

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