Journal
NATURAL PRODUCT RESEARCH
Volume -, Issue -, Pages -Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2023.2275287
Keywords
Oridonin; anticancer; ent-kaurane diterpenoid; derivatives; cytotoxicity
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In this study, researchers designed and synthesized a series of oridonin derivatives and evaluated their bioactivities against various cancer cells. Compound 4b with a 4-fluorophenyl moiety exhibited the highest activity, with an IC50 value of 0.3 mu M against MCF-7 cells, which was 7.4-fold more active than oridonin.
Oridonin is one of the ent-kaurane diterpenes that have been studied extensively for various bioactivities. In an effort to expand natural scaffold-based library as anticancer agents, we have designed and synthesised a number of novel oridonin derivatives and evaluated their bioactivities on a panel of human cancer cell lines (HCT116, A375, MCF-7, HepG2, and A549). Compound 4b bearing a 4-fluorophenyl moiety was found to be the most active compound with an IC50 value of 0.3 mu M against MCF-7 cells, which was 7.4-fold more active than oridonin. This study could provide some insightful information for further synthesis of oridonin derivatives as anticancer agents.
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