Pregled bibliografske jedinice broj: 1139491
Biological activity of newly synthesized benzimidazole and benzothizole 2,5‐disubstituted furane derivatives
Biological activity of newly synthesized benzimidazole and benzothizole 2,5‐disubstituted furane derivatives // Molecules, 26 (2021), 16; 4935, 21 doi:10.3390/molecules26164935 (međunarodna recenzija, članak, znanstveni)
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Naslov
Biological activity of newly synthesized benzimidazole and benzothizole 2,5‐disubstituted furane derivatives
Autori
Racané, Livio ; Zlatar, Ivo ; Perin, Nataša ; Cindrić, Maja ; Radovanović, Vedrana ; Banjanac , Mihailo ; Shanmugam, Suresh ; Radić Stojković, Marijana ; Brajša, Karmen ; Hranjec, Marijana
Izvornik
Molecules (1420-3049) 26
(2021), 16;
4935, 21
Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni
Ključne riječi
amidines ; acrylonitriles ; benzimidazoles ; benzothiazoles ; furanes ; antitumor activity ; DNA binding
Sažetak
Newly designed and synthesized cyano, amidino and acrylonitrile 2, 5‐disubstituted furane derivatives with either benzimidazole/benzothiazole nuclei have been evaluated for antitumor and antimicrobial activity. For potential antitumor activity, the compounds were tested in 2D and 3D cell culture methods on three human lung cancer cell lines, A549, HCC827 and NCI‐H358, with MTS cytotoxicity and BrdU proliferation assays in vitro. Compounds 5, 6, 8, 9 and 15 have been proven to be compounds with potential antitumor activity with high potential to stop the proliferation of cells. In general, benzothiazole derivatives were more active in comparison to benzimidazole derivatives. Antimicrobial activity was evaluated with Broth microdilution testing (according to CLSI (Clinical Laboratory Standards Institute) guidelines) on Gram‐negative Escherichia coli and Gram‐positive Staphylococcus aureus. Additionally, Saccharomyces cerevisiae was included in testing as a eukaryotic model organism. Compounds 5, 6, 8, 9 and 15 showed the most promising antibacterial activity. In general, the compounds showed antitumor activity, higher in 2D assays in comparison with 3D assays, on all three cell lines in both assays. In natural conditions, compounds with such an activity profile (less toxic but still effective against tumor growth) could be promising new antitumor drugs. Some of the tested compounds showed antimicrobial activity. In contrast to ctDNA, the presence of nitro group or chlorine in selected furane‐benzothiazole structures did not influence the binding mode with AT‐DNA. All compounds dominantly bound inside the minor groove of AT‐DNA either in form of monomers or dimer and higher‐order aggregates.
Izvorni jezik
Engleski
Znanstvena područja
Kemija, 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) ( CroRIS)
--IP-2018-01-4694 - Molekularno prepoznavanje DNA:RNA hibridnih i višelančanih struktura u bioanalitičkim i in vitro sustavima (DNARNAHyB-MolBio) (Radić Stojković, Marijana) ( CroRIS)
Ustanove:
Institut "Ruđer Bošković", Zagreb,
Tekstilno-tehnološki fakultet, Zagreb,
Fakultet kemijskog inženjerstva i tehnologije, Zagreb,
Fidelta d.o.o.
Profili:
Marijana Radić Stojković (autor)
Karmen Brajša (autor)
Mihailo Banjanac (autor)
Marijana Hranjec (autor)
Nataša Perin (autor)
Maja Cindrić (autor)
Livio Racane (autor)
Citiraj ovu publikaciju:
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
Uključenost u ostale bibliografske baze podataka::
- CA Search (Chemical Abstracts)