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Pregled bibliografske jedinice broj: 1210082

Harmicens, Novel Harmine and Ferrocene Hybrids: Design, Synthesis and Biological Activity


Poje, Goran; Marinović, Marina; Pavić, Kristina; Mioč, Marija; Kralj, Marijeta; Pessanha de Carvalho, Lais; Held, Jana; Perković, Ivana; Rajić, Zrinka
Harmicens, Novel Harmine and Ferrocene Hybrids: Design, Synthesis and Biological Activity // International journal of molecular sciences, 23 (2022), 9315, 20 doi:10.3390/ijms23169315 (međunarodna recenzija, članak, znanstveni)


CROSBI ID: 1210082 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Harmicens, Novel Harmine and Ferrocene Hybrids: Design, Synthesis and Biological Activity

Autori
Poje, Goran ; Marinović, Marina ; Pavić, Kristina ; Mioč, Marija ; Kralj, Marijeta ; Pessanha de Carvalho, Lais ; Held, Jana ; Perković, Ivana ; Rajić, Zrinka

Izvornik
International journal of molecular sciences (1422-0067) 23 (2022); 9315, 20

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

Ključne riječi
β-carboline ; harmine ; ferrocene ; hybrid ; amide ; triazole ; synthesis ; antiplasmodial ; antiproliferative

Sažetak
Cancer and malaria are both global health threats. Due to the increase in the resistance to the known drugs, research on new active substances is a priority. Here, we present the design, synthesis, and evaluation of the biological activity of harmicens, hybrids composed of covalently bound harmine/β-carboline and ferrocene scaffolds. Structural diversity was achieved by varying the type and length of the linker between the β-carboline ring and ferrocene, as well as its position on the β-carboline ring. Triazole-type harmicens were prepared using Cu(I)-catalyzed azide-alkyne cycloaddition, while the synthesis of amide-type harmicens was carried out by applying a standard coupling reaction. The results of in vitro biological assays showed that the harmicens exerted moderate antiplasmodial activity against the erythrocytic stage of P. falciparum (IC50 in submicromolar and low micromolar range) and significant and selective antiproliferative activity against the MCF-7 and HCT116 cell lines (IC50 in the single-digit micromolar range, SI > 5.9). Cell localization experiments showed different localizations of nonselective harmicene 36 and HCT116- selective compound 28, which clearly entered the nucleus. A cell cycle analysis revealed that selective harmicene 28 had already induced G1 cell cycle arrest after 24 h, followed by G2/M arrest with a concomitant drastic reduction in the percentage of cells in the S phase, whereas the effect of nonselective compound 36 on the cell cycle was much less pronounced, which agreed with their different localizations within the cell.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija, Farmacija



POVEZANOST RADA


Projekti:
UIP-2017-05-5160 - Derivati harmina kao potencijalni antimalarici (CLICKforMALARIA) (Rajić Džolić, Zrinka, HRZZ - 2017-05) ( POIROT)

Ustanove:
Farmaceutsko-biokemijski fakultet, Zagreb,
Institut "Ruđer Bošković", Zagreb

Poveznice na cjeloviti tekst rada:

doi www.mdpi.com doi.org fulir.irb.hr

Citiraj ovu publikaciju:

Poje, Goran; Marinović, Marina; Pavić, Kristina; Mioč, Marija; Kralj, Marijeta; Pessanha de Carvalho, Lais; Held, Jana; Perković, Ivana; Rajić, Zrinka
Harmicens, Novel Harmine and Ferrocene Hybrids: Design, Synthesis and Biological Activity // International journal of molecular sciences, 23 (2022), 9315, 20 doi:10.3390/ijms23169315 (međunarodna recenzija, članak, znanstveni)
Poje, G., Marinović, M., Pavić, K., Mioč, M., Kralj, M., Pessanha de Carvalho, L., Held, J., Perković, I. & Rajić, Z. (2022) Harmicens, Novel Harmine and Ferrocene Hybrids: Design, Synthesis and Biological Activity. International journal of molecular sciences, 23, 9315, 20 doi:10.3390/ijms23169315.
@article{article, author = {Poje, Goran and Marinovi\'{c}, Marina and Pavi\'{c}, Kristina and Mio\v{c}, Marija and Kralj, Marijeta and Pessanha de Carvalho, Lais and Held, Jana and Perkovi\'{c}, Ivana and Raji\'{c}, Zrinka}, year = {2022}, pages = {20}, DOI = {10.3390/ijms23169315}, chapter = {9315}, keywords = {β-carboline, harmine, ferrocene, hybrid, amide, triazole, synthesis, antiplasmodial, antiproliferative}, journal = {International journal of molecular sciences}, doi = {10.3390/ijms23169315}, volume = {23}, issn = {1422-0067}, title = {Harmicens, Novel Harmine and Ferrocene Hybrids: Design, Synthesis and Biological Activity}, keyword = {β-carboline, harmine, ferrocene, hybrid, amide, triazole, synthesis, antiplasmodial, antiproliferative}, chapternumber = {9315} }
@article{article, author = {Poje, Goran and Marinovi\'{c}, Marina and Pavi\'{c}, Kristina and Mio\v{c}, Marija and Kralj, Marijeta and Pessanha de Carvalho, Lais and Held, Jana and Perkovi\'{c}, Ivana and Raji\'{c}, Zrinka}, year = {2022}, pages = {20}, DOI = {10.3390/ijms23169315}, chapter = {9315}, keywords = {β-carboline, harmine, ferrocene, hybrid, amide, triazole, synthesis, antiplasmodial, antiproliferative}, journal = {International journal of molecular sciences}, doi = {10.3390/ijms23169315}, volume = {23}, issn = {1422-0067}, title = {Harmicens, Novel Harmine and Ferrocene Hybrids: Design, Synthesis and Biological Activity}, keyword = {β-carboline, harmine, ferrocene, hybrid, amide, triazole, synthesis, antiplasmodial, antiproliferative}, chapternumber = {9315} }

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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