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Pregled bibliografske jedinice broj: 951028

SAHAquines, Novel Hybrids Based on SAHA and Primaquine Motifs, as Potential Cytostatic and Antiplasmodial Agents


Beus, Maja; Rajić, Zrinka; Maysinger, Dusica; Mlinarić, Zvonimir; Antunović, Maja; Marijanović, Inga; Fontinha, Diana, Prudêncio, Miguel; Held, Jana; Olgen, Sureyya; Zorc; Branka
SAHAquines, Novel Hybrids Based on SAHA and Primaquine Motifs, as Potential Cytostatic and Antiplasmodial Agents // ChemistryOpen, 7 (2018), 624-638 doi:10.1002/open.201800117 (međunarodna recenzija, članak, znanstveni)


CROSBI ID: 951028 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
SAHAquines, Novel Hybrids Based on SAHA and Primaquine Motifs, as Potential Cytostatic and Antiplasmodial Agents

Autori
Beus, Maja ; Rajić, Zrinka ; Maysinger, Dusica ; Mlinarić, Zvonimir ; Antunović, Maja ; Marijanović, Inga ; Fontinha, Diana, Prudêncio, Miguel ; Held, Jana ; Olgen, Sureyya ; Zorc ; Branka

Izvornik
ChemistryOpen (2191-1363) 7 (2018); 624-638

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

Ključne riječi
acetylation ; anticancer agents ; antiplasmodial activity ; cytostatic activity ; drug design

Sažetak
We report the synthesis of SAHAquines and related primaquine (PQ) derivatives. SAHAquines are novel hybrid compounds that combine moieties of suberoylanilide hydroxamic acid (SAHA), an anticancer agent with weak antiplasmodial activity, and PQ, an antimalarial drug with low antiproliferative activity. The preparation of SAHAquines is simple, cheap, and high yielding. It includes the following steps: coupling reaction between primaquine and a dicarboxylic acid monoester, hydrolysis, a new coupling reaction with O‐protected hydroxylamine, and deprotection. SAHAquines 5 a–d showed significant reduction in cell viability. Among the three human cancer cell lines (U2OS, HepG2, and MCF‐7), the most responsive were the MCF‐7 cells. The antibodies against acetylated histone H3K9/H3K14 in MCF‐7 cells revealed a significant enhancement following treatment with N‐hydroxy‐ N′‐{; ; ; ; 4‐[(6‐methoxyquinolin‐8‐ yl)amino]pentyl}; ; ; ; pentanediamide (5 b). Ethyl (2E)‐3‐({; ; ; ; 4‐[(6‐methoxyquinolin‐8‐ yl)amino]pentyl}; ; ; ; carbamoyl)prop‐2‐enoate (2 b) and SAHAquines were the most active compounds against both the hepatic and erythrocytic stages of Plasmodium parasites, some of them at sub‐ micromolar concentrations. The results of our research suggest that SAHAquines are promising leads for new anticancer and antimalarial agents.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija, Farmacija



POVEZANOST RADA


Ustanove
Farmaceutsko-biokemijski fakultet, Zagreb,
Prirodoslovno-matematički fakultet, Zagreb

Profili:

Avatar Url Maja Antunović (autor)

Avatar Url Inga Marijanović (autor)

Avatar Url Zrinka Rajić (autor)

Avatar Url Branka Zorc (autor)

Avatar Url Maja Beus (autor)

Citiraj ovu publikaciju

Beus, Maja; Rajić, Zrinka; Maysinger, Dusica; Mlinarić, Zvonimir; Antunović, Maja; Marijanović, Inga; Fontinha, Diana, Prudêncio, Miguel; Held, Jana; Olgen, Sureyya; Zorc; Branka
SAHAquines, Novel Hybrids Based on SAHA and Primaquine Motifs, as Potential Cytostatic and Antiplasmodial Agents // ChemistryOpen, 7 (2018), 624-638 doi:10.1002/open.201800117 (međunarodna recenzija, članak, znanstveni)
Beus, M., Rajić, Z., Maysinger, D., Mlinarić, Z., Antunović, M., Marijanović, I., Fontinha, Diana, Prudêncio, Miguel, Held, J., Olgen, S., Zorc & Branka (2018) SAHAquines, Novel Hybrids Based on SAHA and Primaquine Motifs, as Potential Cytostatic and Antiplasmodial Agents. ChemistryOpen, 7, 624-638 doi:10.1002/open.201800117.
@article{article, year = {2018}, pages = {624-638}, DOI = {10.1002/open.201800117}, keywords = {acetylation, anticancer agents, antiplasmodial activity, cytostatic activity, drug design}, journal = {ChemistryOpen}, doi = {10.1002/open.201800117}, volume = {7}, issn = {2191-1363}, title = {SAHAquines, Novel Hybrids Based on SAHA and Primaquine Motifs, as Potential Cytostatic and Antiplasmodial Agents}, keyword = {acetylation, anticancer agents, antiplasmodial activity, cytostatic activity, drug design} }

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


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