Pro-apoptotic carboxamide analogues of natural fislatifolic acid targeting Mcl-1 and Bcl-2
| Autor: | Marc Litaudon, Florian Daressy, Kok Hoong Leong, Khalijah Awang, Sandy Desrat, Fanny Roussi, Azhar Ariffin, Shelly Gapil Tiamas, Jérôme Bignon, Alma Abou Samra, Christophe Fourneau, Vincent Steinmetz |
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| Přispěvatelé: | Institut de Chimie des Substances Naturelles (ICSN), Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), University of Malaya [Kuala Lumpur, Malaisie], Institut Gustave Roussy (IGR), Biomolécules : Conception, Isolement, Synthèse (BioCIS), Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Paris-Sud - Paris 11 (UP11)-Université de Cergy Pontoise (UCP), Université Paris-Seine-Université Paris-Seine |
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Cyclohexanecarboxylic Acids
Stereochemistry medicine.drug_class Clinical Biochemistry bcl-X Protein Pharmaceutical Science Carboxamide Antineoplastic Agents Apoptosis 01 natural sciences Biochemistry Small Molecule Libraries chemistry.chemical_compound Cell Line Tumor Drug Discovery medicine Moiety Humans Molecular Biology Cyclohexenyl chalcone Natural product 010405 organic chemistry Chemistry [CHIM.ORGA]Chemical Sciences/Organic chemistry Organic Chemistry Stereoisomerism Affinities Amides Cycloaddition 0104 chemical sciences 3. Good health 010404 medicinal & biomolecular chemistry Molecular Medicine Myeloid Cell Leukemia Sequence 1 Protein Cancer cell lines Drug Screening Assays Antitumor |
| Zdroj: | Bioorganic and Medicinal Chemistry Letters Bioorganic and Medicinal Chemistry Letters, Elsevier, 2020, 30, pp.127003. ⟨10.1016/j.bmcl.2020.127003⟩ |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2020.127003⟩ |
| Popis: | International audience; A library of 26 novel carboxamides deriving from natural fislatifolic acid has been prepared. The synthetic strategy involve dabio-inspired Diels-Aldercycloaddition,followed by functionalisations of the carbonyl moiety. All the compounds were evaluated on Bcl-xL, Mcl-1andBcl-2 proteins. In this series of cyclohexenyl chalcone analogues,six compounds behaved as dua lBcl-xL/Mcl-1 inhibitors in micromolar range and one exhibited sub-micromolar affinities toward Mcl-1andBcl-2.The most potent compounds evaluated on A549 and MCF7cancer cell lines showed moderate cytotoxicities |
| Databáze: | OpenAIRE |
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