AI Article Synopsis
- A collective synthesis of several 4-hydroxy-2-pyridone alkaloids was successfully accomplished, focusing on compounds like pretenellin B and torrubiellone C.
- Key strategies included a strategic convergent synthesis involving Suzuki-Miyaura cross-coupling, and a divergent synthesis using aldol condensation with homologous aldehydes.
- Notably, torrubiellone C exhibited strong inhibitory effects on Jurkat T cells, suggesting potential for drug discovery in creating bioactive small-molecule libraries.
Article Abstract
A collective synthesis of 4-hydroxy-2-pyridone alkaloids--specifically, pretenellin B, prebassianin B, farinosone A, militarione D, pyridovericin, and torrubiellone C--has been achieved. Key steps include using a strategic convergent method to synthesize the densely substituted pyridone key intermediate by Suzuki-Miyaura cross-coupling reaction, a divergent synthesis approach of target molecules by aldol condensation of pyridone intermediate with homologous aldehydes, and an iterative synthesis of homologous aldehydes with all-trans-polyene backbones. Interestingly, among the six tumor cell lines investigated, torrubiellone C was found to induce potent and apoptotic inhibitory activities on Jurkat T cells with IC50 values of 7.05 μM. Hence, this approach could potentially contribute to the synthesis of bioactive small-molecule libraries as well as drug discovery.
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| http://dx.doi.org/10.1002/asia.201402466 | DOI Listing |
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