TY - JOUR 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 SP - 2857 LP - 2868 VL - 25 IS - 4 AU - JOANNA GODLEWSKA AU - WOJCIECH LUNIEWSKI AU - BOGDAN ZAGRODZKI AU - LUKASZ KACZMAREK AU - ALEKSANDRA BIELAWSKA-POHL AU - DANUTA DUS AU - JOANNA WIETRZYK AU - ADAM OPOLSKI AU - MAGDALENA SIWKO AU - ANNA JAROMIN AU - ANNA JAKUBIAK AU - ARKADIUSZ KOZUBEK AU - WANDA PECZYNSKA-CZOCH Y1 - 2005/07/01 UR - http://ar.iiarjournals.org/content/25/4/2857.abstract N2 - 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 ER -