| Abstrak/Abstract |
Synthesis of chalcone and flavone derivatives and its cytotoxicity against cancer
cell lines had been investigated. The chalcone 1a [2'-hydroxy-4-methoxychalcone],
chalcone 1b [2'-hydroxy-3,4-dimethoxychalcone] and chalcone 1c [2'-hydroxy-4- chlorochalcone] were prepared by Claisen-Schmidt condensation of 2- hydroxyacetophenone with 4-methoxybenzaldehyde, 3,4-dimethoxybenzaldehyde,
and 4-chlorobenzaldehyde. Synthesis of chalcones were carried out by stirring at
room temperature for 48 hours using methanol as a solvent and KOH 40% as a
catalyst with 85.30, 83.33, and 84.01% yields respectively as yellow solid.
Furthermore, oxidative cyclization from chalcones (1a - 1c) with iodine as a catalyst
in DMSO resulted flavone 2a [4'-methoxyflavone], flavone 2b [3',4'- dimethoxyflavone], and flavone 2c [4'-chloroflavone] with 83.33, 85.10, and 87.10%
yields respectively as pale yellow solid. The cytotoxicity test indicated that chalcone
1c had good enough activity for inhibiting the growth of HeLa and WiDr cancer cells
with IC50 value 44.67 and 41.67 µg/mL respectively. While flavones (2a –2c) were not
active for inhibiting the growth of HeLa with IC50 value more than 100 µg/mL. |
