Search for content and authors

Disubstituted indolo[2,3-b]quinoline derivatives - the cytotoxic activity in vitro against various human tumor cell lines.

Wojciech Łuniewski 1Marta Świtalska 2Małgorzata Piskozub 2Joanna Wietrzyk 2Łukasz S. Kaczmarek 1Wanda Peczyńska-Czoch 3

1. Pharmaceutical Research Institute (IF), Rydygiera 8, Warszawa 01-793, Poland
2. Polish Academy of Sciences, Institute of Immunology and Experimental Therapy (IITD), Rudolfa Weigla 12, Wrocław 53-114, Poland
3. Wrocław University of Technology, Department of Organic Chemistry, Wybrzeże Wyspiańskiego 27, Wrocław 50-370, Poland


In our study double substituted indolo[2,3-b]quinoline derivatives bearing (dialkylamino)alkyl chains at N-6 and C-2 or C-9 position were tested against various human tumor cell lines and their drug-resistant sublines: human colon cancer (LoVo) and doxorubicin-resistant LoVo/DX (P-gp-dependent, MRP-, LRP-dependent multidrug resistance),  uterine sarcoma (MES-SA) and MES-SA/DX5 (P-gp-dependent resistance to doxorubicin), human promyelocytic leukemia cell line (HL-60) and HL-60/MX2 (P-gp-independent and topoisomerase II-dependent resistance).

The results of our investigations showed that all these compounds were able to overcome the barrier of P-gp-dependent drug resistance. The most effective of the all tested diubstituted indolo[2,3-b]quinoline derivatives were derivatives substituted in position C-2. The tested compounds did not overcome the barrier of topoisomerase II-dependent drug resistance. Only compound ISS-101 showed ability to overcome the barrier of drug resistance against human promyelocytic leukemia cell line.


Legal notice
  • Legal notice:

Related papers

Presentation: Poster at VI Multidyscyplinarna Konferencja Nauki o Leku, by Wojciech Łuniewski
See On-line Journal of VI Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2008-04-07 12:59
Revised:   2009-06-07 00:48