2. Academic Validation
  3. 2-substituted benzothiazoles as antiproliferative agents: Novel insights on structure-activity relationships

2-substituted benzothiazoles as antiproliferative agents: Novel insights on structure-activity relationships

  • Eur J Med Chem. 2020 Dec 1:207:112762. doi: 10.1016/j.ejmech.2020.112762.
Alessandra Ammazzalorso 1,  Simone Carradori 2,  Rosa Amoroso 2,  Inmaculada Fernández Fernández 3
Affiliations

Affiliations

  • 1 Department of Pharmacy, "G. D'Annunzio" University of Chieti-Pescara, Via Dei Vestini 31, 66100, Chieti, Italy. Electronic address: alessandra.ammazzalorso@unich.it.
  • 2 Department of Pharmacy, "G. D'Annunzio" University of Chieti-Pescara, Via Dei Vestini 31, 66100, Chieti, Italy.
  • 3 Departamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, C/Profesor García González, 2, 41012, Sevilla, Spain.
PMID: 32898763 DOI: 10.1016/j.ejmech.2020.112762
Abstract

Given the wide spectrum of biological activities, benzothiazoles represent privileged scaffolds in medicinal chemistry, useful in drug discovery programs to modulate biological activities of lead compounds. A large body of knowledge about benzothiazoles has been reported in scientific literature, describing their antimicrobial, anticonvulsant, neuroprotective, anti-inflammatory, and antiproliferative effects. This review summarizes the results obtained in the structure-activity relationship studies on antiproliferative benzothiazoles, focusing on 2-substituted derivatives and on mechanism of action responsible for the antitumor effects of this class of compounds.

Keywords

Anti-cancer agents; Benzothiazole; Kinase inhibitors; Molecular hybridization; Structure-activity relationships.

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