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Article Abstract
A simple and economical method was developed for the extraction and isolation of pentacyclic triterpenoid lantadene A from the leaves of . The lantadene A displays significant anti-inflammatory and anticancer properties via the inhibition of IKK-mediated NF-κB protein. Therefore, the derivatives of lantadene A were synthesised to further optimise the pharmacophore for anti-inflammatory and anticancer activities. The synthesised compounds were docked into the active site of IKK to find the most potent inhibitor of IKK. Molecular docking studies revealed that 3,22-diisobutyl substituted lantadene derivative () binds to the IKK protein with the highest affinity. Furthermore, in the ADMET studies, the lead IKK inhibitor () was found to be Ames non-toxic, non-carcinogen, and a weak inhibitor of hERG.[Figure: see text].
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| http://dx.doi.org/10.1080/14786419.2020.1752204 | DOI Listing |
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