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Selected Drug-Likeness Properties of 2-Arylidene-indan-1,3-dione Derivatives-Chemical Compounds with Potential Anti-Cancer Activity.
Pluskota, Robert; Jaroch, Karol; Koslinski, Piotr; Ziomkowska, Blanka; Lewinska, Agnieszka; Kruszewski, Stefan; Bojko, Barbara; Koba, Marcin.
Afiliación
  • Pluskota R; Department of Toxicology and Bromatology, Collegium Medicum im. L. Rydygier in Bydgoszcz, Nicolaus Copernicus University, 87-100 Torun, Poland.
  • Jaroch K; Department of Pharmacodynamics and Molecular Pharmacology, Collegium Medicum im. L. Rydygier in Bydgoszcz, Nicolaus Copernicus University, 87-100 Torun, Poland.
  • Koslinski P; Department of Toxicology and Bromatology, Collegium Medicum im. L. Rydygier in Bydgoszcz, Nicolaus Copernicus University, 87-100 Torun, Poland.
  • Ziomkowska B; Department of Biophysics, Collegium Medicum im. L. Rydygier in Bydgoszcz, Nicolaus Copernicus University, 87-100 Torun, Poland.
  • Lewinska A; Faculty of Chemistry, University of Wroclaw, Joliot-Curie 14, 50-383 Wroclaw, Poland.
  • Kruszewski S; Department of Biophysics, Collegium Medicum im. L. Rydygier in Bydgoszcz, Nicolaus Copernicus University, 87-100 Torun, Poland.
  • Bojko B; Department of Pharmacodynamics and Molecular Pharmacology, Collegium Medicum im. L. Rydygier in Bydgoszcz, Nicolaus Copernicus University, 87-100 Torun, Poland.
  • Koba M; Department of Toxicology and Bromatology, Collegium Medicum im. L. Rydygier in Bydgoszcz, Nicolaus Copernicus University, 87-100 Torun, Poland.
Molecules ; 26(17)2021 Aug 30.
Article en En | MEDLINE | ID: mdl-34500689
ABSTRACT
2-Arylidene-indan-1,3-done derivatives have very different properties, thanks to which they find various applications in science, medicine, and industry. Selected derivatives show antiviral, antibacterial, and anti-inflammatory activity. This paper presents a procedure for the synthesis of a series of indan-1,3-dione derivatives that present antiproliferative activity. The aim of the work was to develop a method of simple synthesis and purification, evaluate the fulfillment of the Lipinski's and Veber's rule, and determine the potential scope of application of the obtained series of compounds. The structure of the synthesized compounds was confirmed, and their lipophilicity was determined using experimental and computational methods. Their antiproliferative activity against selected cell lines was tested in accordance with the MTT protocol; the ability to bind to albumin was tested, and the parameters related to the toxicity of substances in silico were determined. The selected compounds which showed antiproliferative activity were strongly bound to albumin and, in most cases, met the Lipinski's and Veber's rule. Thus, the obtained results suggest that 2-arylidene-indan-1,3-done derivatives appear to be good candidates for drugs with a potential leading structure for further development.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antineoplásicos Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2021 Tipo del documento: Article País de afiliación: Polonia

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antineoplásicos Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2021 Tipo del documento: Article País de afiliación: Polonia
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