Ultrasounds-mediated 10-seconds synthesis of chalcones as potential farnesyltransferase inhibitors |
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| Institution: | 1. Yncréa Hauts-de-France, Laboratory of Sustainable Chemistry and Health, Health & Environment Department, Team Sustainable Chemistry, Ecole des Hautes Etudes d’Ingénieur (HEI), UCLille, 13 rue de Toul, F-59046 Lille, France;2. Univ. Lille, Inserm, CHU Lille, Institut Pasteur de Lille, U1167 – RID-AGE – Facteurs de risque et déterminants moléculaires des maladies liées au vieillissement, F-59000 Lille, France;3. Faculté des Sciences Pharmaceutiques et Biologiques de Lille, F-59006 Lille Cedex, France;4. Institut de Chimie des Substances Naturelles, UPR2301 CNRS, Centre de Recherche de Gif, Avenue de la Terrasse, F-91198 Gif-sur-Yvette Cedex, France;5. ‘Al. I. Cuza’ University of Iasi, Faculty of Chemistry, Bd. Carol I, nr. 11, 700506 Iasi, Romania;1. Department of Chemistry, Faculty of Science, King Abdulaziz University, P.O. Box 80203, Jeddah 21589, Saudi Arabia;2. Center of Excellence for Advanced Materials Research (CEAMR), King Abdulaziz University, P.O. Box 80203, Jeddah 21589, Saudi Arabia;3. Department of Applied Science, School of Engineering & Technology, The NorthCap University, Sector 23A, Gurgaon 122017, India;4. Department of Chemistry, Faculty of Science, University of Tabuk, Tabuk, Saudi Arabia;1. Anti-Cancer Drug Screening Facility (ACDSF), Advanced Centre for Treatment, Research & Education in Cancer (ACTREC), Tata Memorial Centre, Kharghar, Navi Mumbai 410210, India;2. Tumor Immunology & Immunotherapy Group, Advanced Centre for Treatment, Research & Education in Cancer (ACTREC), Tata Memorial Centre, Kharghar, Navi Mumbai 410210, India;3. Homi Bhabha National Institute (HBNI), Training School Complex, Anushakti Nagar, Mumbai 400085, India;4. Department of Organic Synthesis and Process Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India;5. Academy of Scientific and Innovative Research (AcSIR), New Delhi 110025, India;6. Small Animal Imaging Facility, Advanced Centre for Treatment, Research & Education in Cancer (ACTREC), Tata Memorial Centre, Kharghar, Navi Mumbai 410210, India;7. Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037, India;8. Molecular Biology Division, Bhabha Atomic Research Centre, Trombay, Mumbai 400 085, India;9. School of Pharmaceutical Education and Research (SPER), Jamia Hamdard, New Delhi 110062, India;10. Department of Humanities and Sciences, Vardhaman College of Engineering (Autonomous), Shamshabad, Hyderabad, Telangana 501218, India;1. State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China;2. College of Chemistry and Chemical Engineering, Jishou University, Jishou, China;3. College of Food Science and Technology, Shanghai Ocean University, Shanghai, China;4. Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang, China;5. School of Pharmacy, Guizhou Medical University, Guiyang, China;1. Institute of Oncology and Radiology of Serbia, Pasterova 14, 11000 Belgrade, Serbia;2. Faculty of Science, Department of Chemistry, University of Kragujevac, R. Domanovica 12, 34000 Kragujevac, Serbia;3. Laboratory for Radiobiology and Molecular Genetics, “Vin?a” Institute of Nuclear Sciences, University of Belgrade, 11000 Belgrade, Serbia;4. Faculty of Pharmacy, Department of Organic Chemistry, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia;1. Division of Drug Design and Medicinal Chemistry Research Lab, Department of Pharmaceutical Chemistry, Ahalia School of Pharmacy, Palakkad 678557, Kerala, India;2. Department of Pharmaceutical Chemistry, Grace College of Pharmacy, Palakkad 678004, Kerala, India;3. Department of Biochemistry, Faculty of Pharmacy, Hacettepe University, 06100 S?hhiye, Ankara, Turkey;4. School of Health Sciences, University of KwaZulu-Natal, Westville, Durban 4001, South Africa;5. The School of Pure & Applied Physics, M.G. University, Kottayam, India;6. Department of Pharmacology, Grace College of Pharmacy, Palakkad 678004, Kerala, India;7. Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi, Jharkhand 835 215, India |
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| Abstract: | A broad range of chalcones and derivatives were easily and rapidly synthesized, following Claisen-Schmidt condensation of (hetero)aryl ketones and (hetero)aryl aldehydes using a ultrasound probe. A comparison was made with classical magnetic stirring experiments, and an optimization study was realized, showing lithium hydroxide to be the best basic catalyst of the studied condensations. By-products of the reactions (β-hydroxy-ketone, diketones, and cyclohexanols) were also isolated. All compounds were evaluated in vitro for their ability to inhibit human farnesyltransferase, a protein implicated in cancer and rare diseases and on the NCI-60 cancer cell lines panel. Molecules showed inhibitory activity on the target protein and cytostatic effect on different cell lines with particular activity against MCF7, breast cancer cells. |
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| Keywords: | Farnesyltransferase Inhibitor Chalcone Claisen-Schmidt Ultrasounds |
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