Synthesis and biological studies of new piperidino-1,2,3-triazole hybrids with 3-aryl isoxazole side chains

Autor: Vennu Narendar, Philippe Juin, A. K. D. Bhavani, Rémy Le Guével, Fabien Gautier, Appala Venkata Ramana Murthy, Nicolas Levoin, Nangunoori Sampath Kumar, René Grée, Chada Raji Reddy, Paul Mosset, Hélène Solhi, Pasula Aparna, Julie Roul
Přispěvatelé: Jawaharlal Nehru Technological University, Hyderabad 500085, India (JNTU), Osmania University, Plate-forme ImPACcell (ImPACcell), Structure Fédérative de Recherche en Biologie et Santé de Rennes ( Biosit : Biologie - Santé - Innovation Technologique ), Centre de Recherche en Cancérologie Nantes-Angers (CRCNA), Centre Hospitalier Universitaire d'Angers (CHU Angers), PRES Université Nantes Angers Le Mans (UNAM)-PRES Université Nantes Angers Le Mans (UNAM)-Hôtel-Dieu de Nantes-Institut National de la Santé et de la Recherche Médicale (INSERM)-Hôpital Laennec-Centre National de la Recherche Scientifique (CNRS)-Faculté de Médecine d'Angers-Centre hospitalier universitaire de Nantes (CHU Nantes), CRLCC René Gauducheau, CSIR Indian Institute of Chemical Technology (IICT), Institut des Sciences Chimiques de Rennes (ISCR), Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-Université de Rennes 1 (UR1), Université de Rennes (UNIV-RENNES)-Université de Rennes (UNIV-RENNES)-Ecole Nationale Supérieure de Chimie de Rennes (ENSCR)-Institut National des Sciences Appliquées - Rennes (INSA Rennes), Institut National des Sciences Appliquées (INSA)-Université de Rennes (UNIV-RENNES)-Institut National des Sciences Appliquées (INSA), Bioprojet-Biotech, Financial support by the 'Ligue contre le Cancer, Conseil Interrégional Grand Ouest' is gratefully acknowledged., Université de Rennes (UR)-Institut National des Sciences Appliquées - Rennes (INSA Rennes), Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Ecole Nationale Supérieure de Chimie de Rennes (ENSCR)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)
Jazyk: angličtina
Rok vydání: 2021
Předmět:
Models
Molecular
1
2
3-Triazole
Cell Survival
Protein-protein interactions
[SDV]Life Sciences [q-bio]
Clinical Biochemistry
Pharmaceutical Science
Antineoplastic Agents
[SDV.CAN]Life Sciences [q-bio]/Cancer
PUMA (p53 upregulated modulator of apoptosis)
01 natural sciences
Biochemistry
Protein–protein interaction
03 medical and health sciences
chemistry.chemical_compound
Structure-Activity Relationship
Piperidines
Cell Line
Tumor
Drug Discovery
Side chain
Humans
[CHIM]Chemical Sciences
Isoxazole
Cytotoxicity
Molecular Biology
030304 developmental biology
Cell Proliferation
Cancer
0303 health sciences
Biological studies
Dose-Response Relationship
Drug
Molecular Structure
010405 organic chemistry
Aryl
Organic Chemistry
Isoxazoles
Triazoles
Combinatorial chemistry
0104 chemical sciences
3. Good health
chemistry
BRET (Bioluminescence Resonance Energy Transfer)
Cancer cell
Molecular Medicine
Molecular modelling
Drug Screening Assays
Antitumor
Bcl-xL (B-cell lymphoma-extra large)
Zdroj: Bioorganic & Medicinal Chemistry Letters
Bioorganic & Medicinal Chemistry Letters, 2021, 52, pp.128390. ⟨10.1016/j.bmcl.2021.128390⟩
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2021.128390⟩
Popis: International audience; A small library of new piperidine-triazole hybrids with 3-aryl isoxazole side chains has been designed and synthesized. Their cytotoxicity against a panel of seven cancer cell lines has been established. For the most promising compound, an IC(50) value of 3.8 μM on PUMA/Bcl-xL interaction in live cancer cells was established through BRET analysis. A rationale was proposed for these results through complete molecular modelling studies.
Databáze: OpenAIRE
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