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2002 | 49 | 1 | 87-92
Article title

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

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Languages of publication
EN
Abstracts
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.
Publisher

Year
Volume
49
Issue
1
Pages
87-92
Physical description
Dates
published
2002
received
2001-09-10
revised
2002-01-20
accepted
2002-02-20
Contributors
  • Department of Pharmaceutical Technology and Biochemistry, Chemical Faculty, Technical University of Gdańsk, Gdańsk, Poland
  • Department of Pharmaceutical Technology and Biochemistry, Chemical Faculty, Technical University of Gdańsk, Gdańsk, Poland
  • Department of Chemical Sciences, University of Camerino, Camerino (MC), Camerino, Italy
  • Department of Pharmaceutical Technology and Biochemistry, Chemical Faculty, Technical University of Gdańsk, Gdańsk, Poland
References
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  • 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. Stefańska, B., Dzieduszycka, M., Bontemps- Gracz, M.M., Borowski, E., Martelli, S., Supino, R., Pratesi, G., De Cesare, M.A., Zunino, F., Kuśnierczyk, 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., Stefańska, 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) Aktywność cytotoksyczna nowych pochodnych i analogów antrachinonu oraz zwiazków pokrewnych z grupy akrydyny ze szczególnym uwzględnieniem komórek nowotworowych z indukowaną krzyżową opornością wielolekową. (The cytotoxic activity of novel derivatives and analogues of anthraquinone 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-(ω-aminoalkyl)-2,6-dihydropyrazolo[3,4,5-kl]- 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(ω-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. 45, 696.
Document Type
Publication order reference
Identifiers
YADDA identifier
bwmeta1.element.bwnjournal-article-abpv49i1p87kz
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