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Insight on [1,3]thiazolo[4,5-e]isoindoles as tubulin polymerization inhibitors

  1. Author:
    Spano, Virginia
    Barreca, Marilia
    Rocca, Roberta
    Bortolozzi, Roberta
    Bai, Ruoli
    Carbone, Anna
    Raimondi, Maria Valeria
    Piccionello, Antonio Palumbo
    Montalbano, Alessandra
    Alcaro, Stefano
    Hamel, Ernest
    Viola, Giampietro
    Barraja, Paola

  2. Author Address

    Univ Palermo, Dipartimento Sci & Tecnol Biol Chim & Farmaceut S, Via Archirafi 32, I-90123 Palermo, Italy.Magna Graecia Univ Catanzaro, Dipartimento Med Sperimentale & Clin, Viale Europa, I-88100 Catanzaro, Italy.Magna Graecia Univ Catanzaro, Net4Sci Srl, Acad Spinoff, Viale Europa, I-88100 Catanzaro, Italy.Fdn Citta Speranza, Ist Ric Pediat IRP, Corso Stati Uniti 4, I-35127 Padua, Italy.NCI, Mol Pharmacol Branch, Dev Therapeut Program,NIH, Div Canc Treatment & Diag,Frederick Natl Lab Canc, Frederick, MD 21702 USA.Magna Graecia Univ Catanzaro, Dipartimento Sci Salute, Viale Europa, I-88100 Catanzaro, Italy.Univ Padua, Lab Oncoematol, Dipartimento Salute Donna & Bambino, Via Giustiniani 2, I-35131 Padua, Italy.Univ Genoa, Dipartimento Farm, Viale Benedetto XV 3, I-16132 Genoa, Italy.
    1. Year: 2021
    2. Date: Feb 15
  2. Journal: European Journal of Medicinal Chemistry
  3. ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER,
    1. 212
  5. Type of Article: Article
  6. Article Number: ARTN 113122
  7. ISSN: 0223-5234
  1. Abstract:

    A series of [1,3]thiazolo[4,5-e]isoindoles has been synthesized through a versatile and high yielding multistep sequence. Evaluation of the antiproliferative activity of the new compounds on the full NCI human tumor cell line panel highlighted several compounds that are able to inhibit tumor cell proliferation at micromolar-submicromolar concentrations. The most active derivative 11g was found to cause cell cycle arrest at the G2/M phase and induce apoptosis in HeLa cells, following the mitochondrial pathway, making it a lead compound for the discovery of new antimitotic drugs. (C) 2020 Elsevier Masson SAS. All rights reserved.

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External Sources

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  2. DOI: 10.1016/j.ejmech.2020.113122
  3. PMID: 33401199
  4. View record in Web of Science®
  5. WOS: 000629622800025

Library Notes

  1. Fiscal Year: FY2020-2021
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