RS6077 induces mitotic arrest and selectively activates cell death in human cancer cell lines and in a lymphoma tumor in vivo.

Humans Apoptosis Cell Death Mitosis HeLa Cells Tubulin / metabolism Lymphoma / drug therapy Cell Line, Tumor Cell Proliferation
Lymphoma Mitotic arrest Pyrrole Synthesis Tubulin

Journal

European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510

Informations de publication

Date de publication:
15 Jan 2023
Historique:
received: 25 05 2022
revised: 20 11 2022
accepted: 29 11 2022
pubmed: 12 12 2022
medline: 4 1 2023
entrez: 11 12 2022
Statut: ppublish

Résumé

We synthesized a new inhibitor of tubulin polymerization, the pyrrole (1-(7H-pyrrolo[2,3- d]pyrimidin-4-yl)-1H-pyrrol-3-yl)(3,4,5-trimethoxy-phenyl)methanone 6 (RS6077). Compound 6 inhibited the growth of multiple cancer cell lines, with IC

Identifiants

DOI: 10.1016/j.ejmech.2022.114997 PMID: 36502578
pubmed: 36502578
pii: S0223-5234(22)00899-6
doi: 10.1016/j.ejmech.2022.114997
pii:
doi:

Substances chimiques

Tubulin 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

114997

Informations de copyright

Copyright © 2022 Elsevier Masson SAS. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Jessica Sebastiani (J)

Laboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy.

Michela Puxeddu (M)

Laboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy.

Marianna Nalli (M)

Laboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy.

Ruoli Bai (R)

Molecular Pharmacology Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, Frederick National Laboratory for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD, 21702, United States.

Ludovica Altieri (L)

Department of Biology and Biotechnology "Charles Darwin", Sapienza University of Rome, Rome, Italy; IBPM Institute of Molecular Biology and Pathology - Consiglio Nazionale Delle Ricerche, Rome, Italy.

Paola Rovella (P)

IBPM Institute of Molecular Biology and Pathology - Consiglio Nazionale Delle Ricerche, Rome, Italy.

Eugenio Gaudio (E)

Institute of Oncology Research, Faculty of Biomedical Sciences, USI, Via Francesco Chiesa 5, 6500, Bellinzona, Switzerland.

Daniela Trisciuoglio (D)

Department of Biology and Biotechnology "Charles Darwin", Sapienza University of Rome, Rome, Italy; IBPM Institute of Molecular Biology and Pathology - Consiglio Nazionale Delle Ricerche, Rome, Italy.

Filippo Spriano (F)

Institute of Oncology Research, Faculty of Biomedical Sciences, USI, Via Francesco Chiesa 5, 6500, Bellinzona, Switzerland.

Patrizia Lavia (P)

Department of Biology and Biotechnology "Charles Darwin", Sapienza University of Rome, Rome, Italy; IBPM Institute of Molecular Biology and Pathology - Consiglio Nazionale Delle Ricerche, Rome, Italy.

Cinzia Fionda (C)

Department of Molecular Medicine, Sapienza University of Rome, Viale Regina Elena 291, 00161, Rome, Italy.

Domiziana Masci (D)

Department of Basic Biotechnological Sciences, Intensivological and Perioperative Clinics, Catholic University of the Sacred Heart, Largo Francesco Vito 1, 00168, Rome, Italy.

Andrea Urbani (A)

Department of Basic Biotechnological Sciences, Intensivological and Perioperative Clinics, Catholic University of the Sacred Heart, Largo Francesco Vito 1, 00168, Rome, Italy.

Chiara Bigogno (C)

Aphad SrL, Via Della Resistenza 65, 20090, Buccinasco, Italy.

Giulio Dondio (G)

Aphad SrL, Via Della Resistenza 65, 20090, Buccinasco, Italy.

Ernest Hamel (E)

Molecular Pharmacology Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, Frederick National Laboratory for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD, 21702, United States.

Francesco Bertoni (F)

Institute of Oncology Research, Faculty of Biomedical Sciences, USI, Via Francesco Chiesa 5, 6500, Bellinzona, Switzerland; Oncology Institute of Southern Switzerland, Ente Ospedaliero Cantonale, 6500, Bellinzona, Switzerland.

Romano Silvestri (R)

Laboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy. Electronic address: romano.silvestri@uniroma1.it.

Giuseppe La Regina (G)

Laboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › RS6077 induces mitotic arrest and selectively...
questionsmedicales.fr › Phénomènes physiologiques cellulaires › Mort cellulaire › Mort cellulaire régulée › Apoptose › RS6077 induces mitotic arrest and selectively...
questionsmedicales.fr › Phénomènes physiologiques cellulaires › Mort cellulaire › RS6077 induces mitotic arrest and selectively...
questionsmedicales.fr › Phénomènes génétiques › Division du noyau cellulaire › Mitose › RS6077 induces mitotic arrest and selectively...
questionsmedicales.fr › Cellules › Cellules épithéliales › Cellules HeLa › RS6077 induces mitotic arrest and selectively...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines de tissu nerveux › Tubuline › RS6077 induces mitotic arrest and selectively...
questionsmedicales.fr › Maladies du système immunitaire › Syndromes immunoprolifératifs › Syndromes lymphoprolifératifs › Lymphomes › RS6077 induces mitotic arrest and selectively...
questionsmedicales.fr › Cellules › Cellules cultivées › Cellules cancéreuses en culture › Lignée cellulaire tumorale › RS6077 induces mitotic arrest and selectively...
questionsmedicales.fr › Phénomènes physiologiques › Croissance et développement › Croissance › Processus de croissance cellulaire › Prolifération cellulaire › RS6077 induces mitotic arrest and selectively...