AI Article Synopsis
- A series of synthesized derivatives of (±)-trans-dihydronarciclasine and (±)-trans-dihydrolycoricidine, focusing on variations in ring A, were tested against 60 human tumor cell lines to evaluate their anti-cancer effects.
- Among the 13 tested alkaloids, (±)-trans-dihydronarciclasine demonstrated the strongest ability to kill cancer cells.
- A structure-activity relationship analysis revealed that a hydroxy group at position 7 and a rigid 1,3-benzodioxole structure are crucial for the antiproliferative effectiveness of these compounds.
Article Abstract
A series of (±)-trans-dihydronarciclasine and (±)-trans-dihydrolycoricidine derivatives with variously substituted ring A was synthesised and evaluated for their antiproliferative activity against 60 human tumour cell lines (NCI60), representing leukemia, melanoma, and cancers of the lung, colon, brain, ovary, breast, prostate, as well as kidney in vitro. Among the 13 alkaloids screened, (±)-trans-dihydronarciclasine showed the highest potency as a cytotoxic molecule. A structure-activity relationship (SAR) study indicated that the presence of a hydroxy group at position 7 and a rigid, 1,3-benzodioxole scaffold were essential for the antiproliferative activity.
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| http://dx.doi.org/10.1016/j.ejmech.2019.04.010 | DOI Listing |
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