Synthesis and Heme Polymerization Inhibitory Activity (HPIA) Assay of Chalcone, Flavone and Flavanone Derivatives

Abstract

Chalcone, flavone, and flavanone had been synthesized as candidate of the antimalarial compounds. The chalcone 1was synthesised from 2,4-dihydroxyacetophenone and 4-metoxybenzaldehyde as starting materials using base catalyst KOH via Claisen-Schmidt Condensation. The synthesis flavone 2was carried out by cyclization of chalcone 1using I2 in DMSO, while the flavanone 3was produced by cyclization of chalcone 1using NaOAc as a base catalyst. An in vitro antimalarial activity of the compound 1, 2and 3have been evaluated with the chloroquine diphosphate as a positive control in various concentration, and this assay was carried out according to the Basilico method. The IC50value of compound 1, 2, 3and a positive control were 0.25; 0.62; 1.33 and 0.35 mM, respectively. The result showed that chalcone1with the lowestIC50value is a potential candidate as an antimalarial agent.

Cytotoxicity Assay of 2,4-Dihydroxide-4’-Methoxychalcone Against Cervical (HeLa) Cancer Cell by MTT Assay

“…The procedure of synthesis of 2,4-dihydroxide-4'-methoxychalcone using the sonochemical method for 7 hours in (Suryani et al, 2019), and all chemicals used purified by column chromatography to yield product and purchased commercially. 2,4dihydroxide-4'-methoxychalcone characterized by FT-IR, GC-MS, 1 H, and 13 C-NMR.…”

“…Then, absorbance reading by ELISA reader at 595 nm (wavelength optimum) and Percentage of survival cells were determined and calculated by eq. The compound of 2,4-dihydroxide-4'-methoxychalcone has been synthesized by (Suryani et al, 2019) with yield product 98 %, respectively. Sonochemical method using to achieve optimal yield and this method an alternative to a short time reaction of synthesis.…”

“…The result showed that the sonochemical method was efficient (Monsef et al, 2020) since the conventional method needs a long time reaction for 24-72 hours. Chalcone compound was identified by spectral data IR, EI-MS, 1 H, and 13 C-NMR (Suryani et al, 2019). By 1 H-NMR, H with 7,44 ppm and H 7,86 ppm with doublet peak (J = 15 Hz) described the unsaturated carbonyl of chalcone were performed.…”