Aim: Synthesis of new heterocyclic chalcone derivatives with promising antitumor activity.
Introduction: Natural chalcones have been intensively studied for their wide range of biological activities, namely antitumor.1 Possessing two electrophilic reactive centers at α,β-unsaturated ketone group, chalcone derivatives can participate in addition reactions leading to the synthesis of promising bioactive compounds with a more rigid structure, like isoxazoles and pyrazoles.2
Methods: Chalcones were synthesized by base catalysed Claisen Schmidt condensation via microwave assisted organic synthesis (MAOS). The antiproliferative activity was assessed using sulforhodamine B assay.3
Results: Seventeen chalcone derivatives were synthesized and identified as having in vitro growth inhibitory activity on three human tumor cell lines from breast, lung and melanoma (MCF-7, NCI-H460, and A375-C5).
Conclusion: Most of the synthetized chalcones revealed to be promising growth inhibitors of human tumor cell lines. The molecular mechanisms involved in their antiproliferative effect are being evaluated.
Acknowledgements: This research was partially supported through national funds provided by FCT, ERDF and COMPETE under the Strategic Funding UID/Multi/04423/2013, and the projects PTDC/MAR-BIO/4694/2014 (POCI-01-0145-FEDER-016790), PTDC/DTPFTO/1981/2014 (POCl-01-0145-FEDER-016581), and PTDC/AAGTEC/0739/2014 (POCI-01-0145-FEDER-016793) in the framework of the programme PT2020 as well as by the project INNOVMAR-Innovation and Sustainability in the Management and Exploitation of Marine Resources (NORTE-01-0145-FEDER-000035, within Research Line NOVELMAR), supported by NORTE 2020, under the PORTUGAL 2020 Partnership Agreement, through the ERDF. Patrícia M.A. Silva is a PhD fellowship holder from FCT (SFRH/BD/90744/2012).