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Pregled bibliografske jedinice broj: 533675

Synthesis, cytostatic activity and ADME properties of C-5 substituted and N-acyclic pyrimidine derivatives

Gazivoda Kraljević, Tatjana; Klika, Mateja; Kralj, Marijeta; Martin-Kleiner, Irena; Jurmanović, Stella; Milić, Astrid; Padovan, Jasna; Raić-Malić, Silvana
Synthesis, cytostatic activity and ADME properties of C-5 substituted and N-acyclic pyrimidine derivatives // Bioorganic & medicinal chemistry letters, 22 (2012), 1; 308-312 doi:10.1016/j.bmcl.2011.11.009 (međunarodna recenzija, članak, znanstveni)

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Naslov
Synthesis, cytostatic activity and ADME properties of C-5 substituted and N-acyclic pyrimidine derivatives

Autori
Gazivoda Kraljević, Tatjana ; Klika, Mateja ; Kralj, Marijeta ; Martin-Kleiner, Irena ; Jurmanović, Stella ; Milić, Astrid ; Padovan, Jasna ; Raić-Malić, Silvana

Izvornik
Bioorganic & medicinal chemistry letters (0960-894X) 22 (2012), 1; 308-312

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

Ključne riječi
5-alkyl pyrimidine derivatives ; cytostatic evaluations ; cell cycle analysis ; ADME properties

Sažetak
The synthesis of the novel 5-alkyl pyrimidine derivatives, 5, 6-dihydrofuro[2, 3-d]pyrimidines and 5-alkyl N-methoxymethyl pyrimidine derivatives and evaluation of their cytostatic activities are described. The mechanism of antiproliferative effect of 5-(2-chloroethyl)-substituted pyrimidine 3 that exerted the pronounced cytostatic activity was studied in further details on colon carcinoma (HCT116) cells. The cell cycle perturbation analysis demonstrated severe DNA damage (G2/M arrest) pointing to a potential DNA alkylating ability of 3. Preliminary ADME data of 3 and its 6-methylated structural congener (6-Me-3) showed their high permeability and good metabolic stability.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti



POVEZANOST RADA

Projekti:
MZOS-098-0982464-2514 - Uloga različitih mehanizama odgovora stanica na terapiju oštećenjem DNA (Kralj, Marijeta, MZOS ) ( CroRIS)
MZOS-125-0982464-2925 - Razvoj i primjena novih molekula u pozitron-emisijskoj tomografiji (PET) (Raić-Malić, Silvana, MZOS ) ( CroRIS)

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

Profili:

Avatar Url Jasna Padovan (autor)

Avatar Url Silvana Raić-Malić (autor)

Avatar Url Irena Martin-Kleiner (autor)

Avatar Url Marijeta Kralj (autor)

Avatar Url Astrid Milić (autor)

Avatar Url Stella Jurmanović (autor)

Avatar Url Tatjana Gazivoda Kraljević (autor)

Poveznice na cjeloviti tekst rada:

doi dx.doi.org www.sciencedirect.com

Citiraj ovu publikaciju:

Gazivoda Kraljević, Tatjana; Klika, Mateja; Kralj, Marijeta; Martin-Kleiner, Irena; Jurmanović, Stella; Milić, Astrid; Padovan, Jasna; Raić-Malić, Silvana
Synthesis, cytostatic activity and ADME properties of C-5 substituted and N-acyclic pyrimidine derivatives // Bioorganic & medicinal chemistry letters, 22 (2012), 1; 308-312 doi:10.1016/j.bmcl.2011.11.009 (međunarodna recenzija, članak, znanstveni)
Gazivoda Kraljević, T., Klika, M., Kralj, M., Martin-Kleiner, I., Jurmanović, S., Milić, A., Padovan, J. & Raić-Malić, S. (2012) Synthesis, cytostatic activity and ADME properties of C-5 substituted and N-acyclic pyrimidine derivatives. Bioorganic & medicinal chemistry letters, 22 (1), 308-312 doi:10.1016/j.bmcl.2011.11.009.
@article{article, author = {Gazivoda Kraljevi\'{c}, Tatjana and Klika, Mateja and Kralj, Marijeta and Martin-Kleiner, Irena and Jurmanovi\'{c}, Stella and Mili\'{c}, Astrid and Padovan, Jasna and Rai\'{c}-Mali\'{c}, Silvana}, year = {2012}, pages = {308-312}, DOI = {10.1016/j.bmcl.2011.11.009}, keywords = {5-alkyl pyrimidine derivatives, cytostatic evaluations, cell cycle analysis, ADME properties}, journal = {Bioorganic and medicinal chemistry letters}, doi = {10.1016/j.bmcl.2011.11.009}, volume = {22}, number = {1}, issn = {0960-894X}, title = {Synthesis, cytostatic activity and ADME properties of C-5 substituted and N-acyclic pyrimidine derivatives}, keyword = {5-alkyl pyrimidine derivatives, cytostatic evaluations, cell cycle analysis, ADME properties} }
@article{article, author = {Gazivoda Kraljevi\'{c}, Tatjana and Klika, Mateja and Kralj, Marijeta and Martin-Kleiner, Irena and Jurmanovi\'{c}, Stella and Mili\'{c}, Astrid and Padovan, Jasna and Rai\'{c}-Mali\'{c}, Silvana}, year = {2012}, pages = {308-312}, DOI = {10.1016/j.bmcl.2011.11.009}, keywords = {5-alkyl pyrimidine derivatives, cytostatic evaluations, cell cycle analysis, ADME properties}, journal = {Bioorganic and medicinal chemistry letters}, doi = {10.1016/j.bmcl.2011.11.009}, volume = {22}, number = {1}, issn = {0960-894X}, title = {Synthesis, cytostatic activity and ADME properties of C-5 substituted and N-acyclic pyrimidine derivatives}, keyword = {5-alkyl pyrimidine derivatives, cytostatic evaluations, cell cycle analysis, ADME properties} }

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::


  • CAB Abstracts
  • CA Search (Chemical Abstracts)
  • EMBASE (Excerpta Medica)
  • Beilstein Database
  • Chemical Citation Index

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