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. 2018 Aug 14;107:615–624. doi: 10.1016/j.biopha.2018.07.147

Table 2.

Synthetic or natural derivatives of lycorine and their anticancer activity compare to lycorine.

Inline graphic
Position Substitution or derivate Activity Ref
Ring-A Open dioxole Moderately active [23]
Open dioxole with absence of -OH at C2 Inactive [23]
Ring-B C7-oxidation, aromatic C-ring Inactive [23,133]
C7-oxidation Decrease [133]
C7-thiol Inactive [133]
Quaternization of N Inactive [23]
Ring-C 1-acetyl Decrease [23,134,135]
1-acetyl, 2-silyl Inactive [134]
1-alkyl, 2-silyl ether Moderately active [86,135]
1-silyl, 2-alkyl ether Inactive [86,134]
2-amines Decrease [136]
2-β acetyl Inactive [23]
2-epoxide Increase [136]
2-esters Decrease [136]
2-methoxy Equipotent [23,134]
1 or 2 methyl ether Inactive [86]
1 or 2 benzoate Equipotent [133]
1, 2-diacetyl Inactive [23,134,135]
1, 2-dicarbonate Equipotent [133]
1, 2-diether Decrease [86]
1,2-dipropionate Equipotent [133]
1,2-disilyl Inactive [134]
1,2,3,4-tetraol Inactive [133]
2.3-diallyl Equipotent [133]
Aromatic C ring Selective [23]
Oxiadation of C3-C4 double bond Inactive [23,136]
Steriochemistry change Inactive [23]
Ring-D (narciclasine type) Narciclasine Equipotent [135,137]
Narciclasine tetraacetate Equipotent [135]
C10b-R-hydroxypancratistatin Moderately active [135]
Cis-dihydronarciclasine Moderately active [135]
Trans-dihydronarciclasine Decrease [135]
Ring-D (crinine type) Haemanthamine Equipotent [135]
Buphanamine Inactive [135]
11-hydroxyvittatine Inactive [135,138,139]
Natural derivatives Pseudolycorine Moderately active [23,135]
Amarbellisine Moderately active [135]
Ungeremine Inactive [23,135]
Norpluiine Inactive [23,135]
Lycorene Inactive [23]