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4 results on '"Mélissa Cucca"'

1. Design, synthesis and biological evaluation of conformationnally-restricted analogues of E7010 as inhibitors of tubulin assembly (ITA) and vascular disrupting agents (VDA)

Author

Vassili Prudhomme, Mélissa Cucca, Lionel Nauton, Elsa Andrieu, Mathilde Fereyrolles, Sylvain Lamoine, Clément Michelin, Khalil Bennis, Aurore Collin, Frédéric De Ceuninck, Iuliana Botez, Christophe Mallet, Sylvie Ducki, Institut de Chimie de Clermont-Ferrand (ICCF), Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Clermont Auvergne (UCA)-Institut national polytechnique Clermont Auvergne (INP Clermont Auvergne), Université Clermont Auvergne (UCA)-Université Clermont Auvergne (UCA), and ANR-16-IDEX-0001,CAP 20-25,CAP 20-25(2016)

Subjects
E7010, Pharmacology, History, Vascular-disrupting agents (VDA), Indoles, Polymers and Plastics, Organic Chemistry, Inhibition of tubulin assembly (ITA), Antineoplastic Agents, Angiogenesis Inhibitors, General Medicine, Industrial and Manufacturing Engineering, Tubulin Modulators, Tubulin, Cell Line, Tumor, Drug Discovery, [CHIM]Chemical Sciences, Business and International Management
Abstract

Vascular-disrupting agents (VDA) specifically target established neovasculature which results in vascular shutdown. This therapeutic strategy could improve the outcome of pathologies involving aberrant angiogenesis. Although several classes of VDA exist, inhibitors of tubulin assembly (ITA) represent the main category. A series of 21 conformationnally-restricted analogues of E7010, a known ITA-VDA, were designed and synthesised as novel inhibitors of tubulin assembly (ITA) and vascular-disrupting agents (VDA). Among them, indole 4j exhibited good potency against HUVEC and HIG-82 cell lines, as well as a good ability to inhibit tubulin assembly. Furthermore, indole 4j reduced HUVEC migration in a dose-dependent manner, indicating a vascular disrupting activity comparable to that of the gold standard, Combretastatin A4 (CA4).

Published
2022
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2. Bioinspired Direct Access to Benzofuroindolines by Oxidative [3 + 2] Annulation of Phenols and Indoles

Author

Rodolphe Beaud, Cyrille Kouklovsky, Guillaume Vincent, Mélissa Cucca, Natacha Denizot, Régis Guillot, and Annie Pouilhes

Subjects
Indole test, Annulation, Indoles, Molecular Structure, Organic Chemistry, Oxidative phosphorylation, Biochemistry, Catalysis, chemistry.chemical_compound, Phenols, chemistry, Electrophile, Organic chemistry, Phenol, Oxidative coupling of methane, Physical and Theoretical Chemistry, Oxidation-Reduction, Benzofurans
Abstract

The straightforward entry to benzofuroindoline containing natural product-like scaffolds has been achieved by a challenging [3 + 2] oxidative coupling between phenols and indoles. The reaction proceeds by NIS-oxidation of the indole followed by the trapping of the resulting electrophilic intermediate by phenol.

Published
2014
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3. Phthalocyanine-chalcone conjugates

Author

Fallia Aribi, Jérémie Fournier-dit-Chabert, Sebile Işık Büyükekşi, Khalil Bennis, Derya Topkaya, Ayşe Gül Gürek, Vefa Ahsen, Devrim Atilla, Charlene Vey, Gökçe Canan Taşkın, Mélissa Cucca, Florian Albrieux, Sinem Tuncel Kostakoğlu, Sylvie Ducki, Serkan Alpugan, Fabienne Dumoulin, Department of chemistry - Gebze Technical University, Gebze Teknik Üniversitesi [Gebze], Institut de Chimie de Clermont-Ferrand (ICCF), Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Centre Commun de Spectrometrie de Masse (CCSM), Institut de Chimie et Biochimie Moléculaires et Supramoléculaires (ICBMS), Université Claude Bernard Lyon 1 (UCBL), Université de Lyon-Université de Lyon-Institut National des Sciences Appliquées de Lyon (INSA Lyon), Université de Lyon-Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Institut de Chimie du CNRS (INC)-École Supérieure Chimie Physique Électronique de Lyon-Centre National de la Recherche Scientifique (CNRS)-Université Claude Bernard Lyon 1 (UCBL), Université de Lyon-Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Institut de Chimie du CNRS (INC)-École Supérieure Chimie Physique Électronique de Lyon-Centre National de la Recherche Scientifique (CNRS), Université de Lyon-Université de Lyon-École Supérieure de Chimie Physique Électronique de Lyon (CPE)-Institut National des Sciences Appliquées de Lyon (INSA Lyon), Université de Lyon-Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Claude Bernard Lyon 1 (UCBL), and Université de Lyon-Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)

Subjects
Chalcone, 010405 organic chemistry, Chemistry, photosensitizer, medicine.medical_treatment, chalcone, Photodynamic therapy, vascular disruption, General Chemistry, 010402 general chemistry, Grafting, Photochemistry, 01 natural sciences, 0104 chemical sciences, chemistry.chemical_compound, phthalocyanine, photodynamic therapy, medicine, Phthalocyanine, [CHIM]Chemical Sciences, Photosensitizer, Conjugate
Abstract

International audience; A phthalocyanine-chalcone conjugate was previously reported to retain the full photodynamic activity of the phthalocyanine and a slightly lowered antivascular effect of the chalcone. Assuming that it was due to an insufficient release of the chalcone, we described here several grafting modes applied to the preparation of phthalocyanine-chalcone conjugates.

Published
2016
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4. ChemInform Abstract: Bioinspired Direct Access to Benzofuroindolines by Oxidative [3 + 2] Annulation of Phenols and Indoles

Author

Régis Guillot, Mélissa Cucca, Natacha Denizot, Cyrille Kouklovsky, Annie Pouilhes, Guillaume Vincent, and Rodolphe Beaud

Subjects
Indole test, chemistry.chemical_compound, Annulation, chemistry, Electrophile, Organic chemistry, Phenol, Oxidative coupling of methane, General Medicine, Phenols, Oxidative phosphorylation
Abstract

The straightforward entry to benzofuroindoline containing natural product-like scaffolds has been achieved by a challenging [3 + 2] oxidative coupling between phenols and indoles. The reaction proceeds by NIS-oxidation of the indole followed by the trapping of the resulting electrophilic intermediate by phenol.

Published
2015
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