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Evaluation of dapsone and its synthetic derivative DDS‑13 in cancer in vitro.
- Source :
-
Experimental & Therapeutic Medicine . Jan2024, Vol. 27 Issue 1, pN.PAG-N.PAG. 1p. - Publication Year :
- 2024
-
Abstract
- The present study highlighted the repositioning of the drug dapsone (DDS) for cancer therapy. Due to its mechanism of action, DDS has a dual effect as an antibiotic and as an anti-inflammatory/immunomodulator; however, at high doses, it has important adverse effects. The derivative DDS-13 [N,N'-(sulfonyl bis (4,1-phenylene)) dioctanamide] was synthesized through an N-acylation reaction to compare it with DDS. Its cytotoxic effects in cancer cells (DU145 and HeLa) and non-cancer cells (HDFa) were observed at concentrations ranging 0.01-100 µM and its physicochemical/pharmacokinetic properties were analyzed using the SwissADME tool. The objectives of the present study were to evaluate the anticancer activity of both DDS and DDS-13 and to identify the physicochemical and pharmacokinetic properties of DDS-13. The results showed that DDS-13 presented a cytotoxic effect in the DU145 cell line (IC50=19.06 µM), while DDS showed a cytotoxic effect on both the DU145 (IC50=11.11 µM) and HeLa (IC50=13.07 µM) cell lines. DDS-13 appears to be a good cytotoxic candidate for the treatment of prostate cancer, while DDS appears to be a good candidate for both cervical and prostate cancer. Neither candidate showed a cytotoxic effect in non-cancerous cells. The different pharmacokinetic properties of DDS-13 make it a new candidate for evaluation in preclinical models for the treatment of cancer. [ABSTRACT FROM AUTHOR]
- Subjects :
- *DAPSONE
*DRUG repositioning
*PROSTATE cancer
*CELL lines
*PHARMACOKINETICS
Subjects
Details
- Language :
- English
- ISSN :
- 17920981
- Volume :
- 27
- Issue :
- 1
- Database :
- Academic Search Index
- Journal :
- Experimental & Therapeutic Medicine
- Publication Type :
- Academic Journal
- Accession number :
- 174790618
- Full Text :
- https://doi.org/10.3892/etm.2023.12335