AI Article Synopsis
- A study explored 3-chloropiperidines as sustainable anticancer agents, synthesizing various monofunctional compounds efficiently and in high yields.
- These compounds demonstrated strong DNA alkylation and low nanomolar cytotoxicity against carcinoma cell lines, particularly pancreatic cancer, outperforming the standard drug chlorambucil.
- Stereochemistry affected the activity of these compounds, indicating potential additional mechanisms of action, making them promising candidates for future anticancer drug development.
Article Abstract
The pressing demand for sustainable antitumor drugs prompted us to investigate 3-chloropiperidines as potential mustard-based anticancer agents. In this study, an explorative set of variously decorated monofunctional 3-chloropiperidines (M-CePs) was efficiently synthesized through a fast and affordable route providing high yields of pure racemates and enantiomers. Consistently with their reactivity, M-CePs were demonstrated to alkylate DNA . On a panel of carcinoma cell lines, M-CePs exhibited low nanomolar cytotoxicity indexes, which showed their remarkable activity against pancreatic cancer cells and in all cases performed strikingly better than the chlorambucil control. Very interestingly, stereochemistry modulated the activity of M-CePs in unexpected ways, pointing to additional molecular mechanisms of action beyond the direct damage of genomic DNA. This encouraging combination of efficacy and sustainability suggests they are valid candidates for anticancer agent development.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6466835 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.8b00580 | DOI Listing |
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