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

Authors :
Heise, Niels V.
Meyer, Sven J.
Csuk, René
Mueller, Thomas
Source :
European Journal of Medicinal Chemistry. Oct2024, Vol. 276, pN.PAG-N.PAG. 1p.
Publication Year :
2024

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 IC 50 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. [Display omitted] • Dehydroabietylamine was converted into a sulfonamide/rhodamine B conjugate. • This conjugate was tested for cytotoxic activity with a panel of human cancer cells. • This conjugate as well as a cyclododecyl analog held IC 50 < 1 μM. • Both conjugates were able to overcome drug resistance and accumulated intracellular. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
02235234
Volume :
276
Database :
Academic Search Index
Journal :
European Journal of Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
178886120
Full Text :
https://doi.org/10.1016/j.ejmech.2024.116667