Synthesis of Some Chalcone Derivatives, in vitro and in Silico Toxicity Evaluation

• Main Authors: A. N. Kristanti, Hery Suwito, Nanik Siti Aminah, K.U. Haq, Helda Dwi Hardiyanti, H. Anggraeni, N. Faiza, R.S. Anto, S. Muharromah
• Format: Article PeerReviewed
• Language: English; English; English; English
• Published: Rasayan Journal 2020
• Subjects: Q Science; Q Science (General); QD Chemistry
• Online Access: http://repository.unair.ac.id/98015/1/C09.%20Abstract.pdf; http://repository.unair.ac.id/98015/2/C09.%20Fulltext%20-%20SYNTHESIS_RASAYAN.pdf; http://repository.unair.ac.id/98015/3/C09.%20Peerreviewer%20-%20Synthesis%20of%20Some%20Chalcone%20Derivatives.pdf; http://repository.unair.ac.id/98015/4/C09.%20Similarity%20-%20SYNTHESIS_RASAYAN%20-%20Copy.pdf; http://repository.unair.ac.id/98015/; http://dx.doi.org/10.31788/RJC.2020.1315534
• Institution: Universitas Airlangga

Chalcone can be synthesized using some methods, but conventional Claisen-Schmidt condensation is still the bestmethod. The objevtives of this study were to synthesize some chalcone derivatives using conventional ClaisenSchmidt condensation by reacting 2-hydroxyacetophenone and some substituted benzaldehydes using NaOH 40%, followed by evaluating their cytotoxicity in vitro against HeLa cancer cells line using MTT method and analyzing molecular docking on p53 and MDM2 interaction. Cytotoxicity test exhibited that 2,5-dimethoxy-2´- hydroxychalcone and 4-chloro-2'-hydroxychalcone gave very low IC50, but both did not show potential apoptosis activity, while in docking analysis 4-chloro-2'-hydroxychalcone showing the best results.