2024

  • [DOI] Lamaa, D.; Cailleau, C.; Vergnaud, J.; Mougin, J.; Bignon, J.; Alami, M.; Fattal, E.; Hamze, A.; Tsapis, N.. Overcoming Solubility Challenges: Liposomal Isocoq‐carbazole as a Promising Anti‐tumor Agent for Inoperable and Radiation‐insensitive Cancers. ChemBioChem 2024. doi:10.1002/cbic.202400062
  • [DOI] Abbouchi, A. E.; Mkhayar, K.; Elkhattabi, S.; Brahmi, N. E.; Hiebel, M.-A.; Bignon, J.; Guillaumet, G.; Suzenet, F.; Kazzouli, S. E.. Design, Synthesis, Computational Studies, and Anti-proliferative Evaluation of Novel Ethacrynic Acid Derivatives Containing Nitrogen Heterocycle, Urea, and Thiourea Moieties as Anticancer Agents. Molecules 2024, 29 (7), 1437. doi:10.3390/molecules29071437
  • [DOI] Michel, L.; Auvray, M.; Askenatzis, L.; Badet-Denisot, M.-A.; Bignon, J.; Durand, P.; Mahuteau-Betzer, F.; Chevalier, A.. Visualization of an Endogenous Mitochondrial Azoreductase Activity Under Normoxic Conditions Using a Naphthalimide Azo-based Fluorogenic Probe. Analytical Chemistry 2024. doi:10.1021/acs.analchem.3c05030

2023

  • [DOI] Loarer, A. L.; Dufossé, L.; Bignon, J.; Frédérich, M.; Ledoux, A.; Fouillaud, M.; Gauvin-Bialecki, A.. OSMAC Method to Assess Impact of Culture Parameters on Metabolomic Diversity and Biological Activity of Marine-derived Actinobacteria. Marine Drugs 2023, 22 (1), 23. doi:10.3390/md22010023
  • [DOI] Alami, O.; Laurent, R.; Tassé, M.; Coppel, Y.; Collière, V.; Bignon, J.; Majoral, J.-P.; Kazzouli, S.; Brahmi, N.; Caminade, A.-M.. Functionalization of Graphene Oxide Surfaces with Phosphorus Dendrimer and Dendron. FlatChem 2023, 42, 100564. doi:10.1016/j.flatc.2023.100564
  • [DOI] Alami, O.; Laurent, R.; Tassé, M.; Coppel, Y.; Bignon, J.; Kazzouli, S.; Majoral, J.-P.; Brahmi, N.; Caminade, A.-M.. “click”chemistry for the Functionalization of Graphene Oxide with Phosphorus Dendrons: Synthesis, Characterization and Preliminary Biological Properties. Chemistry – A European Journal 2023. doi:10.1002/chem.202302198
  • [DOI] Jézéquel, G.; Rampal, C.; Guimard, C.; Kovacs, D.; Polidori, J.; Bigay, J.; Bignon, J.; Askenatzis, L.; Litaudon, M.; Pham, V.-C.; Huong, D.; Nguyen, A.; Pruvost, A.; Virolle, T.; Mesmin, B.; Desrat, S.; Antonny, B.; Roussi, F.. Structure-based Design of a Lead Compound Derived from Natural Schweinfurthins with Antitumor Properties That Target Oxysterol-binding Protein. Journal of Medicinal Chemistry 2023, 66 (20), 14208–14220. doi:10.1021/acs.jmedchem.3c01298
  • [DOI] Losa, R.; Lorton, C.; Retailleau, P.; Bignon, J.; Voituriez, A.. Fluorinated 2-azetines: Synthesis, Applications, Biological Tests, and Development of a Catalytic Process. Organic Letters 2023, 25 (27), 5140–5144. doi:10.1021/acs.orglett.3c01888
  • [DOI] Jia, T.; Diane, O.; Ghosh, D.; Skander, M.; Fontaine, G.; Retailleau, P.; Poupon, J.; Bignon, J.; Siasia, Y.; Servajean, V.; Hue, N.; Betzer, J.-F.; Marinetti, A.; Bombard, S.. Anti-cancer and Radio-sensitizing Properties of New Bimetallic (n-heterocyclic Carbene)-amine-pt(ii) Complexes. Journal of Medicinal Chemistry 2023, 66 (10), 6836–6848. doi:10.1021/acs.jmedchem.3c00267
  • [DOI] Loarer, A.; Marcellin-Gros, R.; Dufossé, L.; Bignon, J.; Frédérich, M.; Ledoux, A.; Queiroz, E.; Wolfender, J.-L.; Gauvin-Bialecki, A.; Fouillaud, M.. Prioritization of Microorganisms Isolated from the Indian Ocean Sponge Scopalina Hapalia Based on Metabolomic Diversity and Biological Activity for the Discovery of Natural Products. Microorganisms 2023, 11 (3), 697. doi:10.3390/microorganisms11030697
  • [DOI] Abbouchi, A.; Brahmi, N.; Hiebel, M.-A.; Ghammaz, H.; Fahime, E.; Bignon, J.; Guillaumet, G.; Suzenet, F.; Kazzouli, S.. Improvement of the Chemical Reactivity of Michael Acceptor of Ethacrynic Acid Correlates with Antiproliferative Activities. Molecules 2023, 28 (2), 910. doi:10.3390/molecules28020910

2022

  • [DOI] Keflee, R.; Leong, K.; Ogawa, S.; Bignon, J.; Chan, M.; Kong, K.. Overview of the Multifaceted Resistances Toward Egfr-tkis and New Chemotherapeutic Strategies in Non-small Cell Lung Cancer. Biochemical Pharmacology 2022, 205, 115262. doi:10.1016/j.bcp.2022.115262
  • [DOI] Abdoul-Latif, F.; Elmi, A.; Merito, A.; Nour, M.; Risler, A.; Ainane, A.; Bignon, J.; Ainane, T.. Essential Oil of Ruta Chalepensis L. From Djibouti: Chemical Analysis and Modeling of in Vitro Anticancer Profiling. Separations 2022, 9 (12), 387. doi:10.3390/separations9120387
  • [DOI] Hauguel, C.; Ducellier, S.; Provot, O.; Ibrahim, N.; Lamaa, D.; Balcerowiak, C.; Letribot, B.; Nascimento, M.; Blanchard, V.; Askenatzis, L.; Levaique, H.; Bignon, J.; Baschieri, F.; Bauvais, C.; Bollot, G.; Renko, D.; Deroussent, A.; Prost, B.; Laisne, M.-C.; Michallet, S.; Lafanechère, L.; Papot, S.; Montagnac, G.; Tran, C.; Alami, M.; Apcher, S.; Hamze, A.. Design, Synthesis and Biological Evaluation of Quinoline-2-carbonitrile-based Hydroxamic Acids as Dual Tubulin Polymerization and Histone Deacetylases Inhibitors. European Journal of Medicinal Chemistry 2022, 240, 114573. doi:10.1016/j.ejmech.2022.114573
  • [DOI] Abdoul-Latif, F.; Elmi, A.; Merito, A.; Nour, M.; Risler, A.; Ainane, A.; Bignon, J.; Ainane, T.. Essential Oils of Ocimum Basilicum L. And Ocimum Americanum L. From Djibouti: Chemical Composition, Antimicrobial and Cytotoxicity Evaluations. Processes 2022, 10 (9), 1785. doi:10.3390/pr10091785
  • [DOI] Abdoul-Latif, F.; Elmi, A.; Merito, A.; Nour, M.; Risler, A.; Ainane, A.; Bignon, J.; Ainane, T.. Essential Oils of Tagetes Minuta and Lavandula Coronopifolia from Djibouti: Chemical Composition, Antibacterial Activity and Cytotoxic Activity Against Various Human Cancer Cell Lines. International Journal of Plant Biology 2022, 13 (3), 315–329. doi:10.3390/ijpb13030026
  • [DOI] Abdoul-Latif, F.; Elmi, A.; Merito, A.; Nour, M.; Risler, A.; Ainane, A.; Bignon, J.; Ainane, T.. Chemical Analysis of Essential Oils of Cymbopogon Schoenanthus (L.) Spreng. And Nepeta Azurea R.br. Ex Benth from Djbouti, In-vitro Cytotoxicity Against Cancer Cell Lines and Antibacterial Activities. Applied Sciences 2022, 12 (17), 8699. doi:10.3390/app12178699
  • [DOI] Hauguel, C.; Tran, C.; Provot, O.; Bignon, J.; Gandon, V.; Hamze, A.. Water‐facilitated Nitromethane‐mediated Cyclization of 2‐(phenylvinyl)benzhydrols: Access to 1,3‐diphenyl‐1h‐indenes with Antitumor Activity. Advanced Synthesis & Catalysis 2022, 364 (17), 3004–3015. doi:10.1002/adsc.202200550
  • [DOI] Yan, J.; Tran, C.; Bignon, J.; Provot, O.; Hamze, A.. Synthesis of Dihydro-5h-benzo[c]-fluorenes, Dihydroindeno[c]-chromenes and Thiochromenesviaintramolecular Cyclization and Their Effect on Human Leukemia Cells. Advanced Synthesis & Catalysis 2022, 364 (9), 1613–1619. doi:10.1002/adsc.202200153

2021

  • [DOI] Pecnard, S.; Hamze, A.; Bignon, J.; Prost, B.; Deroussent, A.; Gallego-Yerga, L.; Peláez, R.; Paik, J.; Diederich, M.; Alami, M.; Provot, O.. Anticancer Properties of Indole Derivatives as IsoCombretastatin A-4 Analogues. European Journal of Medicinal Chemistry 2021, 223, 113656. doi:10.1016/j.ejmech.2021.113656
  • [DOI] Abbouchi, A.; Brahmi, N.; Hiebel, M.-A.; Bignon, J.; Guillaumet, G.; Suzenet, F.; Kazzouli, S.. Synthesis and Evaluation of a Novel Class of Ethacrynic Acid Derivatives Containing Triazoles as Potent Anticancer Agents. 2021, 115, 105293. doi:10.1016/j.bioorg.2021.105293
  • [DOI] Mignani, S.; Bignon, J.; Shi, X.; Majoral, J.-P.. First-in-class Phosphorus Dendritic Framework, a Wide Surface Functional Group Palette Bringing Noteworthy Anti-cancer and Anti-tuberculosis Activities: What Lessons to Learn?. Molecules 2021, 26 (12), 3708. doi:10.3390/molecules26123708
  • [DOI] Renault, K.; Chevalier, A.; Bignon, J.; Jacquemin, D.; Richard, J.-A.; Romieu, A.. Coumarin-pyronin Hybrid Dyes: Synthesis, Fluorescence Properties and Theoretical Calculations. ChemPhotoChem 2021. doi:10.1002/cptc.202100069
  • [DOI] Daressy, F.; Malard, F.; Seguy, L.; Guérineau, V.; Apel, C.; Dumontet, V.; Robert, A.; Groo, A.-C.; Litaudon, M.; Bignon, J.; Desrat, S.; Malzert-Fréon, A.; Wiels, J.; Lescop, E.; Roussi, F.. Drimane Derivatives as the First Examples of Covalent BH 3 Mimetics That Target MCL -1. ChemMedChem 2021. doi:10.1002/cmdc.202100011
  • [DOI] Levaique, H.; Pamlard, O.; Apel, C.; Bignon, J.; Arriola, M.; Kuhner, R.; Awang, K.; Loiseau, P.; Litaudon, M.; Pomel, S.. Alkyl-resorcinol Derivatives as Inhibitors of GDP -mannose Pyrophosphorylase with Antileishmanial Activities. Molecules 2021, 26 (6), 1551. doi:10.3390/molecules26061551
  • [DOI] Pecnard, S.; Provot, O.; Levaique, H.; Bignon, J.; Askenatzis, L.; Saller, F.; Borgel, D.; Michallet, S.; Laisne, M.-C.; Lafanechère, L.; Alami, M.; Hamze, A.. Cyclic Bridged Analogs of isoCA -4: Design, Synthesis and Biological Evaluation. European Journal of Medicinal Chemistry 2021, 209, 112873. doi:10.1016/j.ejmech.2020.112873
  • [DOI] Qiu, J.; Chen, L.; Zhan, M.; Laurent, R.; Bignon, J.; Mignani, S.; Shi, X.; Caminade, A.-M.; Majoral, J.-P.. Facile Synthesis of Amphiphilic Fluorescent Phosphorus Dendron-based Micelles as Antiproliferative Agents: First Investigations. Bioconjugate Chemistry 2021, 32 (2), 339–349. doi:10.1021/acs.bioconjchem.0c00716
  • [DOI] Juillet, C.; Ermolenko, L.; Boyarskaya, D.; Baratte, B.; Josselin, B.; Nedev, H.; Bach, S.; Iorga, B.; Bignon, J.; Ruchaud, S.; Al-Mourabit, A.. From Synthetic Simplified Marine Metabolite Analogues to New Selective Allosteric Inhibitor of Aurora B Kinase. Journal of Medicinal Chemistry 2021, 64 (2), 1197–1219. doi:10.1021/acs.jmedchem.0c02064
  • [DOI] Cacheux, F.; Goff, G.; Ouazzani, J.; Bignon, J.; Retailleau, P.; Marinetti, A.; Voituriez, A.; Betzer, J.-F.. The Piancatelli Rearrangement of Non-symmetrical Furan-2,5-dicarbinols for the Synthesis of Highly Functionalized Cyclopentenones. Org. Chem. Front. 2021, 8, 2. doi:10.1039/d1qo00268f
  • [DOI] Hoang, M.-D.; Bodin, J.-B.; Savina, F.; Steinmetz, V.; Bignon, J.; Durand, P.; Clavier, G.; Méallet-Renault, R.; Chevalier, A.. "cinnapht" Dyes: A New Cinnoline/naphthalimide Fused Hybrid Fluorophore. Synthesis, Photo-physical Study and Use for Bio-imaging. RSC Advances 2021, 11 (48), 30088–30092. doi:10.1039/d1ra05110e
  • [DOI] Paysant, H.; Hedir, S.; Justaud, F.; Weiswald, L.; Dine, A.; Soulieman, A.; Hachem, A.; Elie, N.; Brotin, E.; Denoyelle, C.; Bignon, J.; Roussi, F.; Jouanne, M.; Tasseau, O.; Roisnel, T.; Voisin-Chiret, A.; Grée, R.; Levoin, N.; Poulain, L.. Structural Revision of the Mcl-1 Inhibitor MIM 1: Synthesis and Biological Studies on Ovarian Cancer Cells with Evaluation of Designed Analogues. 2021, 19 (41), 8968–8987. doi:10.1039/d1ob01521d

2020

  • [DOI] El-Khoury, F.; Bignon, J.; Martin, J.-R.. Jouvence, a New Human snoRNA Involved in the Control of Cell Proliferation. BMC Genomics 2020, 21 (1). doi:10.1186/s12864-020-07197-3
  • [DOI] Abbouchi, A.; Brahmi, N.; Hiebel, M.-A.; Bignon, J.; Guillaumet, G.; Suzenet, F.; Kazzouli, S.. Synthesis and Biological Evaluation of Ethacrynic Acid Derivatives Bearing Sulfonamides as Potent Anti-cancer Agents. Bioorganic & Medicinal Chemistry Letters 2020, 30 (19), 127426. doi:10.1016/j.bmcl.2020.127426
  • [DOI] Ibrahim, N.; Bonnet, P.; Brion, J.-D.; Peyrat, J.-F.; Bignon, J.; Levaique, H.; Josselin, B.; Robert, T.; Colas, P.; Bach, S.; Messaoudi, S.; Alami, M.; Hamze, A.. Identification of a New Series of Flavopiridol-like Structures as Kinase Inhibitors with High Cytotoxic Potency. European Journal of Medicinal Chemistry 2020, 199, 112355. doi:10.1016/j.ejmech.2020.112355
  • [DOI] Hassane, C.; Fouillaud, M.; Goff, G.; Sklirou, A.; Boyer, J.; Trougakos, I.; Jerabek, M.; Bignon, J.; Voogd, N.; Ouazzani, J.; Gauvin-Bialecki, A.; Dufossé, L.. Microorganisms Associated with the Marine Sponge Scopalina Hapalia: A Reservoir of Bioactive Molecules to Slow down the Aging Process. Microorganisms 2020, 8 (9), 1262. doi:10.3390/microorganisms8091262
  • [DOI] Campos, P.-E.; Herbette, G.; Chendo, C.; Clerc, P.; Tintillier, F.; Voogd, N.; Papanagnou, E.-D.; Trougakos, I.; Jerabek, M.; Bignon, J.; Goff, G.; Ouazzani, J.; Gauvin-Bialecki, A.. Osirisynes G-I, New Long-chain Highly Oxygenated Polyacetylenes from the Mayotte Marine Sponge Haliclona Sp.. Marine Drugs 2020, 18 (7), 350. doi:10.3390/md18070350
  • [DOI] Zhang, K.; Bouakher, A.; Lévaique, H.; Bignon, J.; Retailleau, P.; Alami, M.; Hamze, A.. Imidazodipyridines via DMAP Catalyzed Domino N-H Carbonylation and 6π-electrocyclization: Synthetic Scope and Application. Advanced Synthesis & Catalysis 2020, 362 (15), 3243–3256. doi:10.1002/adsc.202000553
  • [DOI] Khelifi, I.; Pecnard, S.; Bernadat, G.; Bignon, J.; Levaique, H.; Dubois, J.; Provot, O.; Alami, M.. Synthesis and Anticancer Properties of Oxazepines Related to Azaisoerianin and IsoCoQuines. ChemMedChem 2020, 15 (16), 1571–1578. doi:10.1002/cmdc.202000197
  • [DOI] Chen, L.; Fan, Y.; Qiu, J.; Laurent, R.; Li, J.; Bignon, J.; Mignani, S.; Caminade, A.-M.; Shi, X.; Majoral, J.-P.. Potent Anticancer Efficacy of First-in-class Cu II and Au III Metaled Phosphorus Dendrons with Distinct Cell Death Pathways. Chemistry – A European Journal 2020, 26 (26), 5903–5910. doi:10.1002/chem.202001014
  • [DOI] Tiamas, S.; Daressy, F.; Samra, A.; Bignon, J.; Steinmetz, V.; Litaudon, M.; Fourneau, C.; Leong, K.; Ariffin, A.; Awang, K.; Desrat, S.; Roussi, F.. Pro-apoptotic Carboxamide Analogues of Natural Fislatifolic Acid Targeting Mcl-1 and Bcl-2. Bioorganic & Medicinal Chemistry Letters 2020, 30 (7), 127003. doi:10.1016/j.bmcl.2020.127003
  • [DOI] Péresse, T.; Kovacs, D.; Subra, M.; Bigay, J.; Tsai, M.-C.; Polidori, J.; Gautier, R.; Desrat, S.; Fleuriot, L.; Debayle, D.; Litaudon, M.; Pham, V.-C.; Bignon, J.; Antonny, B.; Roussi, F.; Mesmin, B.. Molecular and Cellular Dissection of the Oxysterol-binding Protein Cycle Through a Fluorescent Inhibitor. Journal of Biological Chemistry 2020, 295 (13), 4277–4288. doi:10.1074/jbc.ra119.012012

2019

  • [DOI] Zhang, K.; Bouakher, A.; Levaique, H.; Bignon, J.; Retailleau, P.; Alami, M.; Hamze, A.. Pyrrolo-imidazo[1,2-a]pyridine Scaffolds Through a Sequential Coupling of N-tosylhydrazones with Imidazopyridines and Reductive Cadogan Annulation, Synthetic Scope, and Application. The Journal of Organic Chemistry 2019, 84 (21), 13807–13823. doi:10.1021/acs.joc.9b02018
  • [DOI] Khelifi, I.; Naret, T.; Hamze, A.; Bignon, J.; Levaique, H.; Alvarez, M.; Dubois, J.; Provot, O.; Alami, M.. N,n-bis-heteroaryl Methylamines: Potent Anti-mitotic and Highly Cytotoxic Agents. European Journal of Medicinal Chemistry 2019, 168, 176–188. doi:10.1016/j.ejmech.2019.02.038
  • [DOI] Naret, T.; Khelifi, I.; Provot, O.; Bignon, J.; Levaique, H.; Dubois, J.; Souce, M.; Kasselouri, A.; Deroussent, A.; Paci, A.; Varela, P.; Gigant, B.; Alami, M.; Hamze, A.. 1,1-diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation. Journal of Medicinal Chemistry 2019, 62 (4), 1902–1916. doi:10.1021/acs.jmedchem.8b01386

2018

  • [DOI] Zhao, G.; Bignon, J.; Levaique, H.; Dubois, J.; Alami, M.; Provot, O.. One-pot Synthesis of 2-styrylindoles from Ortho-substituted Chloroenynes. The Journal of Organic Chemistry 2018, 83 (24), 15323–15332. doi:10.1021/acs.joc.8b02563
  • [DOI] Samra, A.; Robert, A.; Gov, C.; Favre, L.; Eloy, L.; Jacquet, E.; Bignon, J.; Wiels, J.; Desrat, S.; Roussi, F.. Dual Inhibitors of the Pro-survival Proteins Bcl-2 and Mcl-1 Derived from Natural Compound Meiogynin A. European Journal of Medicinal Chemistry 2018, 148, 26–38. doi:10.1016/j.ejmech.2018.01.100
  • [DOI] Apel, C.; Bignon, J.; Garcia-Alvarez, M.; Ciccone, S.; Clerc, P.; Grondin, I.; Girard-Valenciennes, E.; Smadja, J.; Lopes, P.; Frédérich, M.; Roussi, F.; Meinnel, T.; Giglione, C.; Litaudon, M.. N-myristoyltransferases Inhibitory Activity of Ellagitannins from Terminalia Bentzoë (L.) L. F. Subsp. Bentzoë. Fitoterapia 2018, 131, 91–95. doi:10.1016/j.fitote.2018.10.014
  • [DOI] Gicquel, M.; Gomez, C.; Alvarez, M.; Pamlard, O.; Guerineau, V.; Jacquet, E.; Bignon, J.; Voituriez, A.; Marinetti, A.. Inhibition of P53-murine Double Minute 2 (MDM2) Interactions with 3,3'-spirocyclopentene Oxindole Derivatives. Journal of medicinal chemistry 2018, 61 (20), 9386–9392. doi:10.1021/acs.jmedchem.8b01137
  • [DOI] Lamaa, D.; Lin, H.-P.; Zig, L.; Bauvais, C.; Bollot, G.; Bignon, J.; Levaique, H.; Pamlard, O.; Dubois, J.; Ouaissi, M.; Souce, M.; Kasselouri, A.; Saller, F.; Borgel, D.; Jayat-Vignoles, C.; Al-Mouhammad, H.; Feuillard, J.; Benihoud, K.; Alami, M.; Hamze, A.. Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on Iso-combretastatin A-4. Journal of Medicinal Chemistry 2018, 61 (15), 6574–6591. doi:10.1021/acs.jmedchem.8b00050
  • [DOI] Nguyen, T.; Nokin, M.; Egorov, M.; Tome, M.; Bodineau, C.; Primo, C.; Minder, L.; Wdzieczak-Bakala, J.; Garcia-Alvarez, M.; Bignon, J.; Thoison, O.; Delpech, B.; Surpateanu, G.; Frapart, Y.; Peyrot, F.; Abbas, K.; Teres, S.; Evrard, S.; Khatib, A.; Soubeyran, P.; Iorga, B.; Duran, R.; Collin, P.. Mtorinhibition via Displacement of Phosphatidic Acid Induces Enhanced Cytotoxicity Specifically in Cancer Cells. Cancer Research 2018, 78 (18), 5384–5397. doi:10.1158/0008-5472.can-18-0232
  • [DOI] Shelly, G.; Audet, F.; Alma, A.; Bignon, J.; Litaudon, M.; Fourneau, C.; Ariffin, A.; Awang, K.; Desrat, S.; Roussi, F.. Asymmetric Total Synthesis and Biological Evaluation of Proapoptotic Natural Myrcene‐derived Cyclohexenyl Chalcones. European Journal of Organic Chemistry 2018. doi:10.1002/ejoc.201800262
  • [DOI] Naret, T.; Bignon, J.; Bernadat, G.; Benchekroun, M.; Levaique, H.; Lenoir, C.; Dubois, J.; Pruvost, A.; Saller, F.; Borgel, D.; Manoury, B.; Leblais, V.; Darrigrand, R.; Apcher, S.; Brion, J.-D.; Schmitt, E.; Leroux, F.; Alami, M.; Hamze, A.. A Fluorine Scan of a Tubulin Polymerization Inhibitor Isocombretastatin A-4: Design, Synthesis, Molecular Modelling, and Biological Evaluation. European Journal of Medicinal Chemistry 2018, 143, 473–490. doi:10.1016/j.ejmech.2017.11.055