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Biomimetic semi-synthesis, structural optimization and anti-HIV activity of naturally scarce Eupholathone-, Lathyranone- and Integerrimine-type Euphorbia Diterpenoids
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DOI：10.1016/j.bmc.2025.118516.png)
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Abstract
En 中文
• The structural modifications of three classes of naturally rare Euphorbia diterpenoids via a biomimetic skeleton conversion strategy was achieved. • The eupholathone esters exhibited the most potent anti-HIV activity, emerging as a promising class of anti-HIV agents within the Euphorbia diterpenoids family. • The structure-activity relationship revealed that acylation of the 6-OH significantly enhanced anti-HIV activity of eupholathone diterpenoids. • The eupholathone ester 2 t showed the best anti-HIV-1 activity, with an EC50 of 1.51 μM and a selectivity index of more than 66.2.
Journal
B
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3
Papers:
1.7W
Citations:
2.7W
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