期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 20, 期 29, 页码 8904-8908出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201403024
关键词
antiproliferation; cell cycle; isoprene units; methylation reactions; resveratrol
资金
- National Natural Science Foundation of China [21172101, 81271421]
- 111 Project
Four novel compounds were designed by tailoring 3,3'-dihydroxyisorenieratene (a natural carotenoid) based on an isoprene unit retention truncation strategy. Among them, the smallest molecule 1 (2,3,6,2', 3', 6'-hexamethyl-4,4'-dihydroxy-trans-stilbene) was concisely synthesized in a one-pot Stille-Heck tandem sequence, and surfaced as a promising lead molecule in terms of its selective antiproliferative activity mediated by blocking the NCI-H460 cell cycle in G1 phase. Additionally, theoretical calculations and cell uptake experiments indicate that the unique polymethylation pattern of compound 1 significantly induces a conformational change shift out of planarity and increases its cell uptake and metabolic stability. The observation should be helpful to rationally design resveratrol-inspired antiproliferative agents.
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