A Pt(IV) Prodrug Combining Chlorambucil and Cisplatin: A Dual-Acting Weapon for Targeting DNA in Cancer Cells
Abstract
:1. Introduction
2. Results and Discussion
2.1. Synthesis and Characterization
2.2. Reduction Studies
2.3. Cytotoxicity Studies
2.4. Cellular Uptake and DNA Platination
2.5. DNA Fragmentation and Apoptosis Induction
3. Materials and Methods
3.1. Synthesis
3.2. Biological Methods
4. Conclusions
Supplementary Materials
Author Contributions
Funding
Acknowledgments
Conflicts of Interest
References
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Compound | IC50 (µM) ± SD | |||||||
---|---|---|---|---|---|---|---|---|
PSN1 | 2008 | C13* | LoVo | A431 | BxPC3 | HCT-15 | BCPAP | |
1 | 0.42 ± 0.1 | 0.31 ± 0.1 | 0.28 ± 0.1 | 0.98 ± 0.1 | 0.41 ± 0.1 | 1.74 ± 0.5 | 0.39 ± 0.1 | 0.51 ± 0.2 |
Chlorambucil | >100 | 34.58 ± 16.5 | >100 | >100 | 74.48 ± 8.2 | >100 | 44.52 ± 9.5 | >100 |
CDDP | 18.11 ± 3.2 | 2.18 ± 0.9 | 22.11 ± 3.2 | 9.15 ± 2.1 | 2.21 ± 0.4 | 7.22 ± 2.2 | 15.28 ± 2.6 | 7.31 ± 1.2 |
IC50 (µM) ± SD | |||
---|---|---|---|
1 | CDDP | OXP | |
HCT-15 | 40.4 ± 5.1 | 71.1 ± 3.9 | 33.2 ± 4.6 |
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Montagner, D.; Tolan, D.; Andriollo, E.; Gandin, V.; Marzano, C. A Pt(IV) Prodrug Combining Chlorambucil and Cisplatin: A Dual-Acting Weapon for Targeting DNA in Cancer Cells. Int. J. Mol. Sci. 2018, 19, 3775. https://doi.org/10.3390/ijms19123775
Montagner D, Tolan D, Andriollo E, Gandin V, Marzano C. A Pt(IV) Prodrug Combining Chlorambucil and Cisplatin: A Dual-Acting Weapon for Targeting DNA in Cancer Cells. International Journal of Molecular Sciences. 2018; 19(12):3775. https://doi.org/10.3390/ijms19123775
Chicago/Turabian StyleMontagner, Diego, Dina Tolan, Emma Andriollo, Valentina Gandin, and Cristina Marzano. 2018. "A Pt(IV) Prodrug Combining Chlorambucil and Cisplatin: A Dual-Acting Weapon for Targeting DNA in Cancer Cells" International Journal of Molecular Sciences 19, no. 12: 3775. https://doi.org/10.3390/ijms19123775