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2002 | 49 | 1 |
Tytuł artykułu

The ability to overcome multidrug resistance of tumour cell lines by novel acridine cytostatics with condensed heterocyclic rings

Warianty tytułu
Języki publikacji
EN
Abstrakty
EN
Two recently synthesized groups of acridine cytostatics containing fused hetero­cyclic ring(s): pyrazoloacridines (PAC) and pyrazolopyrimidoacridines (PPAC) were tested in regard to their in vitro cytotoxic activity towards a panel of sensitive and re­sistant human tumor cell lines. The obtained results corroborate our earlier hypothe­sis on the essential role of heterocyclic ring fused to the acridine moiety in the ability of acridine cytostatics to overcome multidrug resistance of tumor cells. The presence, location and kind of substituents considerably influenced both the cytotoxic activity of the derivatives and their ability to overcome multidrug resistance. The same factors also affected the cytostatics ability to differentiate between tumor cell lines with vari­ous types of drug exporting pumps.
Wydawca
-
Rocznik
Tom
49
Numer
1
Opis fizyczny
p.87-92,fig.
Twórcy
  • Technical University of Gdansk, Gdansk, Poland
autor
autor
autor
Bibliografia
  • 1. Dicato, M., Duhem, C., Pauly, M. & Ries, F. (1997) Multidrug resistance: Molecular and clinical aspects. Cytokines Cell. Mol. Ther. 3, 91-99.
  • 2. Ling, V. (1997) Multidrug resistance: Molecular mechanisms and clinical relevance. Cancer Chemother. Pharmacol. 40(Suppl), S3-S8.
  • 3. van den Heuvel-Eibrink, M.M., Sonneveld, P. & Pieters, R. (2000) The prognostic significance of membrane-transport- associated multidrug resistance (MDR) proteins in leukemia. Int. J. Clin. Pharmacol. Therapeut. 38, 94-110.
  • 4. Stefanska, B., Dzieduszycka, M., Bontemps- Gracz, M.M., Borowski, E., Martelli, S., Supino, R., Pratesi, G., De Cesare, M.A., Zunino, F., Kusnierczyk, H. & Radzikowski, C. (1999) 8,11-Dihydroxy-6-[(aminoalkyl)amino]- 7 H- benzo[e]perimidin-7-ones with activity in multidrug resistant cell lines; synthesis and antitumor evaluation. J. Med. Chem. 42, 3494-3501.
  • 5. Tkaczyk-Gobis, K., Tarasiuk, J., Seksek, O., Stefanska, B., Borowski, E. & Garnier- Suillerot, A. (2000) Transport of new non- cross-resistant antitumor compounds of the benzoperimidine family in multidrug resistant cells. Eur. J. Pharmacol. 413, 131-141.
  • 6. Bontemps-Gracz, M.M. (2000) Aktywnosc cytotoksyczna nowych pochodnych i analogow antrachinonu oraz zwiazkow pokrewnych z grupy akrydyny ze szczegolnym uwzglednieniem komorek nowotworowych z indukowana krzyzowa opornoscia wielolekowa. (The cytotoxic activity of novel derivatives and analogues ofanthraquinone and related acridine compounds with particular emphasis on tumor cell lines with induced multidrug cross-resistance.) Ph.D. Thesis, Gdansk, 2000 (in Polish).
  • 7. Antonini, I., Polucci, P. & Martelli, S. (1999) Preparation of pyrazoloacridines and pyrazolopyrimidoacridines as antitumor agents. PCT Int. Appl. WO 9906405, Chem. Abstr. 130, 153666.
  • 8. Antonini, I., Polucci, P., Magnano, A. & Martelli, S. (2001) Synthesis, antitumor cytotoxicity, and DNA-binding of novel N-5,2-di- (omega -aminoalkyl)-2,6-dihydropyrazolo[3,4,5-k/j- acridine-5-carboxamides. J. Med. Chem. 44, 3329-3333.
  • 9. Antonini, I., Polucci, P., Magnano, A., Gatto, B., Palumbo, M., Menta, E., Pescalli, N. & Martelli, S. (2002) 2,6- Di(omega-aminoalkyl) -2 2,5,6,7-tetrahydropyrazolo[3,4,5-mn]pyrimido- [5,6,1-de]acridine-5,7-diones: Novel, potent, cytotoxic, and DNA-binding agents . J. Med. Chem. (in press).
Typ dokumentu
Bibliografia
Identyfikatory
Identyfikator YADDA
bwmeta1.element.agro-article-3f74c45b-e9b2-4b71-8367-9036421ce3cc
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