AI Article Synopsis
- Researchers synthesized 35 C1,C2-ether analogues of the alkaloid lycorine, which is known for its potential as an anticancer agent.
- The new compounds were tested for their ability to inhibit the growth of various tumor cell lines, showing different resistance to cell death (apoptosis).
- A significant link was found between the compounds' lipophilicity (fat-solubility) and their anticancer effectiveness, suggesting that how well these compounds can penetrate cells is crucial for their design and effectiveness; a theoretical model supports these findings.
Article Abstract
As a continuation of the studies aimed at the development of new anticancer agents derived from the Amaryllidaceae alkaloid lycorine, 35 C1,C2-ether analogues of this natural product were synthesized. The compounds were evaluated for antiproliferative activities in vitro in a panel of tumor cell lines with varied levels of apoptosis resistance. A strong correlation between the compound lipophilicity and anticancer activity was observed, indicating that cell permeability properties must be an important determinant in the design of lycorine-based anticancer agents. A theoretical docking model, consistent with the experimental observations, is presented.
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| http://dx.doi.org/10.1016/j.bmcl.2013.12.073 | DOI Listing |
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