{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,26]],"date-time":"2026-08-26T08:45:51Z","timestamp":1787733951716,"version":"build-2784847793"},"reference-count":40,"publisher":"MDPI AG","issue":"8","license":[{"start":{"date-parts":[[2024,4,17]],"date-time":"2024-04-17T00:00:00Z","timestamp":1713312000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Region Occitanie (France)","award":["00090086\/21012467"],"award-info":[{"award-number":["00090086\/21012467"]}]},{"name":"CNRS, University Paul Sabatier, and IMT Mines Albi","award":["00090086\/21012467"],"award-info":[{"award-number":["00090086\/21012467"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Chalcones are polyphenols that belong to the flavonoids family, known for their broad pharmacological properties. They have thus attracted the attention of chemists for their obtention and potential activities. In our study, a library of compounds from 2\u2032-hydroxychalcone\u2019s family was first synthesized. A one-step mechanochemical synthesis via Claisen\u2013Schmidt condensation reaction under ball mill conditions was studied, first in a model reaction between a 5\u2032-fluoro-2\u2032-hydroxyacetophenone and 3,4-dimethoxybenzaldehyde. The reaction was optimized in terms of catalysts, ratio of reagents, reaction time, and influence of additives. Among all assays, we retained the best one, which gave the highest yield of 96% when operating in the presence of 1 + 1 eq. of substituted benzaldehyde and 2 eq. of KOH under two grinding cycles of 30 min. Thus, this protocol was adopted for the synthesis of the selected library of 2\u2032-hydroxychalcones derivatives. The biological activities of 17 compounds were then assessed against Plasmodium falciparum, Leishmania donovani parasite development, as well as IGR-39 melanoma cell lines by inhibiting their viability and proliferation. Compounds 6 and 11 are the most potent against L. donovani, exhibiting IC50 values of 2.33 \u00b5M and 2.82 \u00b5M, respectively, better than the reference drug Miltefosine (3.66 \u00b5M). Compound 15 presented the most interesting antimalarial activity against the 3D7 strain, with IC50 = 3.21 \u00b5M. Finally, chalcone 12 gave the best result against IGR-39 melanoma cell lines, with an IC50 value of 12 \u00b5M better than the reference drug Dacarbazine (IC50 = 25 \u00b5M).<\/jats:p>","DOI":"10.3390\/molecules29081819","type":"journal-article","created":{"date-parts":[[2024,4,17]],"date-time":"2024-04-17T07:54:36Z","timestamp":1713340476000},"page":"1819","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":3,"title":["The Synthesis of 2\u2032-Hydroxychalcones under Ball Mill Conditions and Their Biological Activities"],"prefix":"10.3390","volume":"29","author":[{"given":"Imen","family":"Abid","sequence":"first","affiliation":[{"name":"LCC (Laboratoire de Chimie de Coordination), UPR CNRS 8241, Universit\u00e9 de Toulouse, UPS, INPT, Inserm ERL 1289, 205 Route de Narbonne, BP 44099, CEDEX 4, F-31077 Toulouse, France"},{"name":"Centre RAPSODEE (Recherche d\u2019Albi en g\u00e9nie des Proc\u00e9d\u00e9s des SOlides Divis\u00e9s, de l\u2019Energie et de l\u2019Environnement), IMT Mines Albi, UMR CNRS 5302, Universit\u00e9 de Toulouse, Campus Jarlard, All\u00e9e des Sciences, CEDEX 09, F-81013 Albi, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wassim","family":"Moslah","sequence":"additional","affiliation":[{"name":"Laboratoire des Biomolecules, Venins et Applications Th\u00e9ranostiques (LR20IPT01), Institut Pasteur de Tunis, Universit\u00e9 Tunis-ElManar, Tunis 1002, Tunisia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sandrine","family":"Cojean","sequence":"additional","affiliation":[{"name":"BioCIS (Biomol\u00e9cules: Conception, Isolement et Synth\u00e8se), UMR CNRS 8076, Universit\u00e9 Paris-Saclay, F-91400 Orsay, France"},{"name":"National Malaria Reference Centre, AP-HP, H\u00f4pital Bichat\u2014Claude Bernard, 46 Rue Henri Huchard, F-75018 Paris, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Nicolas","family":"Imbert","sequence":"additional","affiliation":[{"name":"BioCIS (Biomol\u00e9cules: Conception, Isolement et Synth\u00e8se), UMR CNRS 8076, Universit\u00e9 Paris-Saclay, F-91400 Orsay, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8542-6793","authenticated-orcid":false,"given":"Philippe M.","family":"Loiseau","sequence":"additional","affiliation":[{"name":"BioCIS (Biomol\u00e9cules: Conception, Isolement et Synth\u00e8se), UMR CNRS 8076, Universit\u00e9 Paris-Saclay, F-91400 Orsay, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2060-1837","authenticated-orcid":false,"given":"Alain","family":"Chamayou","sequence":"additional","affiliation":[{"name":"Centre RAPSODEE (Recherche d\u2019Albi en g\u00e9nie des Proc\u00e9d\u00e9s des SOlides Divis\u00e9s, de l\u2019Energie et de l\u2019Environnement), IMT Mines Albi, UMR CNRS 5302, Universit\u00e9 de Toulouse, Campus Jarlard, All\u00e9e des Sciences, CEDEX 09, F-81013 Albi, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Najet","family":"Srairi-Abid","sequence":"additional","affiliation":[{"name":"Laboratoire des Biomolecules, Venins et Applications Th\u00e9ranostiques (LR20IPT01), Institut Pasteur de Tunis, Universit\u00e9 Tunis-ElManar, Tunis 1002, Tunisia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rachel","family":"Calvet","sequence":"additional","affiliation":[{"name":"Centre RAPSODEE (Recherche d\u2019Albi en g\u00e9nie des Proc\u00e9d\u00e9s des SOlides Divis\u00e9s, de l\u2019Energie et de l\u2019Environnement), IMT Mines Albi, UMR CNRS 5302, Universit\u00e9 de Toulouse, Campus Jarlard, All\u00e9e des Sciences, CEDEX 09, F-81013 Albi, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8785-7095","authenticated-orcid":false,"given":"Michel","family":"Baltas","sequence":"additional","affiliation":[{"name":"LCC (Laboratoire de Chimie de Coordination), UPR CNRS 8241, Universit\u00e9 de Toulouse, UPS, INPT, Inserm ERL 1289, 205 Route de Narbonne, BP 44099, CEDEX 4, F-31077 Toulouse, France"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2024,4,17]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"87","DOI":"10.3389\/fnut.2018.00087","article-title":"The Role of Polyphenols in Human Health and Food Systems: A Mini-Review","volume":"5","author":"Cory","year":"2018","journal-title":"Front. 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