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Pregled bibliografske jedinice broj: 1207112

Imidazo[4,5-b]pyridine derived tubulin polymerization inhibitors: Design, synthesis, biological activity in vitro and computational analysis


Boček, Ida; Hok, Lucija; Persoons, Leentje; Daelemans, Dirk; Vianello, Robert; Hranjec, Marijana
Imidazo[4,5-b]pyridine derived tubulin polymerization inhibitors: Design, synthesis, biological activity in vitro and computational analysis // Bioorganic chemistry, 127 (2022), 106032, 13 doi:10.1016/j.bioorg.2022.106032 (međunarodna recenzija, članak, znanstveni)


CROSBI ID: 1207112 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Imidazo[4,5-b]pyridine derived tubulin polymerization inhibitors: Design, synthesis, biological activity in vitro and computational analysis

Autori
Boček, Ida ; Hok, Lucija ; Persoons, Leentje ; Daelemans, Dirk ; Vianello, Robert ; Hranjec, Marijana

Izvornik
Bioorganic chemistry (0045-2068) 127 (2022); 106032, 13

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
acrylonitriles ; amination ; antiproliferative activity in vitro ; imidazo[4, 5-b]pyridine ; docking simulations ; molecular dynamic simulations ; tubulin polymerization

Sažetak
Imidazo[4, 5-b]pyridine derived acrylonitriles were synthesized and explored for their in vitro antiproliferative effect on a diverse human cancer cell line panel. Three compounds, 20, 21 and 33, showed strong activity in the submicromolar range (IC50 0.2–0.6 μM), and were chosen for further biological experiments. Immunofluorescence staining and tubulin polymerization assays confirmed tubulin as the main target, but excluded its colchicine-binding site as a potential interacting unit. This was supported by the computational analysis, which revealed that the most potent ligands act on the extended colchicine site on the surface between interacting tubulin subunits, where they interfere with their polymerization and reveal pronounced antitumor properties. In addition, lead molecule 21 potently inhibited cancer cell migration, while it did not affect the viability of normal cells even at the highest concentration tested (100 μM).

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija, Temeljne medicinske znanosti



POVEZANOST RADA


Projekti:
HRZZ-IP-2018-01-4379 - Istraživanje antioksidativnog djelovanja benzazolskog skeleta u dizajnu novih antitumorskih agensa (AntioxPot) (Hranjec, Marijana, HRZZ - 2018-01) ( POIROT)

Ustanove:
Institut "Ruđer Bošković", Zagreb,
Fakultet kemijskog inženjerstva i tehnologije, Zagreb

Poveznice na cjeloviti tekst rada:

doi www.sciencedirect.com dx.doi.org

Citiraj ovu publikaciju:

Boček, Ida; Hok, Lucija; Persoons, Leentje; Daelemans, Dirk; Vianello, Robert; Hranjec, Marijana
Imidazo[4,5-b]pyridine derived tubulin polymerization inhibitors: Design, synthesis, biological activity in vitro and computational analysis // Bioorganic chemistry, 127 (2022), 106032, 13 doi:10.1016/j.bioorg.2022.106032 (međunarodna recenzija, članak, znanstveni)
Boček, I., Hok, L., Persoons, L., Daelemans, D., Vianello, R. & Hranjec, M. (2022) Imidazo[4,5-b]pyridine derived tubulin polymerization inhibitors: Design, synthesis, biological activity in vitro and computational analysis. Bioorganic chemistry, 127, 106032, 13 doi:10.1016/j.bioorg.2022.106032.
@article{article, author = {Bo\v{c}ek, Ida and Hok, Lucija and Persoons, Leentje and Daelemans, Dirk and Vianello, Robert and Hranjec, Marijana}, year = {2022}, pages = {13}, DOI = {10.1016/j.bioorg.2022.106032}, chapter = {106032}, keywords = {acrylonitriles, amination, antiproliferative activity in vitro, imidazo[4, 5-b]pyridine, docking simulations, molecular dynamic simulations, tubulin polymerization}, journal = {Bioorganic chemistry}, doi = {10.1016/j.bioorg.2022.106032}, volume = {127}, issn = {0045-2068}, title = {Imidazo[4,5-b]pyridine derived tubulin polymerization inhibitors: Design, synthesis, biological activity in vitro and computational analysis}, keyword = {acrylonitriles, amination, antiproliferative activity in vitro, imidazo[4, 5-b]pyridine, docking simulations, molecular dynamic simulations, tubulin polymerization}, chapternumber = {106032} }
@article{article, author = {Bo\v{c}ek, Ida and Hok, Lucija and Persoons, Leentje and Daelemans, Dirk and Vianello, Robert and Hranjec, Marijana}, year = {2022}, pages = {13}, DOI = {10.1016/j.bioorg.2022.106032}, chapter = {106032}, keywords = {acrylonitriles, amination, antiproliferative activity in vitro, imidazo[4, 5-b]pyridine, docking simulations, molecular dynamic simulations, tubulin polymerization}, journal = {Bioorganic chemistry}, doi = {10.1016/j.bioorg.2022.106032}, volume = {127}, issn = {0045-2068}, title = {Imidazo[4,5-b]pyridine derived tubulin polymerization inhibitors: Design, synthesis, biological activity in vitro and computational analysis}, keyword = {acrylonitriles, amination, antiproliferative activity in vitro, imidazo[4, 5-b]pyridine, docking simulations, molecular dynamic simulations, tubulin polymerization}, chapternumber = {106032} }

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE


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