Microbial transformation of azacarbazoles X: Regioselective hydroxylation of 5,11-dimethyl-5H-indolo [2,3-b]quinoline, a novel DNA topoisomerase II inhibitor, by Rhizopus arrhizus期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

Microbial transformation of azacarbazoles X: Regioselective hydroxylation of 5,11-dimethyl-5H-indolo [2,3-b]quinoline, a novel DNA topoisomerase II inhibitor, by Rhizopus arrhizus

Authors:	Wanda Peczyńska-Czoch Jarosław Osiadacz Łukasz Kaczmarek Tomasz Żal

Affiliation:	(1) Institute of Organic Chemistry, Biochemistry, and Biotechnology, Technical University of Wrocaw, 27 Wybrzee Wyspiaskiego, 50-370 Wrocaw, Poland;(2) Pharmaceutical Research Institute, 8 Rydygiera, 01-793 Warszawa, Poland;(3) Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Czerska 12, 53-114 Wrocaw, Poland

Abstract:	Summary Microbial transformation of cytotoxic 5,11-dimethyl-5H-indolo[2,3-b]quinoline (a compound displaying antitumor activity and affecting the activity of calf thymus DNA topoisomerase II) was performed by the Rhizopus arrhizus strain and yielded a 9-hydroxy derivative. The metabolite obtained displayed a stronger cytotoxity against KB cells than the parent compound (ID₅₀=0.001 mol/mL), and stimulated also the formation of calf thymus topoisomerase II mediated pSP65 DNA cleavage in vitro at the concentration of 3 M. Being analogous to 9-hydroxyellipticine (which is an antitumor alkaloid), this novel indolo[2,3-b] quinoline derivative can be regarded as a novel potential antitumor agent.

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