RT Journal Article
SR Electronic
T1 Biological Evaluation of ω-(Dialkylamino)alkyl Derivatives of 6H-indolo[2,3-b]quinoline - Novel Cytotoxic DNA Topoisomerase II Inhibitors
JF Anticancer Research
JO Anticancer Res
FD International Institute of Anticancer Research
SP 2857
OP 2868
VO 25
IS 4
A1 GODLEWSKA, JOANNA
A1 LUNIEWSKI, WOJCIECH
A1 ZAGRODZKI, BOGDAN
A1 KACZMAREK, LUKASZ
A1 BIELAWSKA-POHL, ALEKSANDRA
A1 DUS, DANUTA
A1 WIETRZYK, JOANNA
A1 OPOLSKI, ADAM
A1 SIWKO, MAGDALENA
A1 JAROMIN, ANNA
A1 JAKUBIAK, ANNA
A1 KOZUBEK, ARKADIUSZ
A1 PECZYNSKA-CZOCH, WANDA
YR 2005
UL http://ar.iiarjournals.org/content/25/4/2857.abstract
AB A series of novel 6H-indolo[2,3-b]quinoline derivatives, substituted at C-2, C-9 or N-6 position with dialkyl(alkylamino)alkyl chains differing in the number of methylene groups, was prepared. These compounds were evaluated in vitro for their antimicrobial and cytotoxic activity against several cell lines of different origin and tested for their ability to influence the cell cycle and inhibit topoisomerase II activity. Liphophilic and calf thymus DNA-binding properties of these compounds were also investigated. All the compounds tested inhibited the growth of Gram-positive bacteria and fungi at MIC values ranging between 0.25 and 1 mM. They also showed cytotoxic activity against KB (human cervix carcinoma) cells (ID50 varied from 2.1 to 9.0 μM) and were able to overcome multidrug resistance in colorectal adenocarcinoma LoVo/DX, uterine sarcoma MES-SA/DX5 and promyelocytic leukemia HL-60/MX2 cells (the values of the resistance index RI fell between 0.54 and 2.4). The compounds induced G2M-phase cell cycle arrest in Jurkat T-cell leukemia cells, revealed DNA-binding properties and inhibited topoisomerase II activity. Copyright© 2005 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved