Microbial transformation of azacarbazoles X: Regioselective hydroxylation of 5,11-dimethyl-5H-indolo [2,3-b]quinoline, a novel DNA topoisomerase II inhibitor, byRhizopus arrhizus
✍ Scribed by Wanda Peczyńska-Czoch; Jarosław Osiadacz; Łukasz Kaczmarek; Tomasz Żal
- Book ID
- 104633210
- Publisher
- Springer Netherlands
- Year
- 1996
- Tongue
- English
- Weight
- 387 KB
- Volume
- 18
- Category
- Article
- ISSN
- 0141-5492
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✦ Synopsis
Microbial transformation of cytotoxic 5,1 l-dimethyl-5H-indolo [2,3-b]quinoline (a compound displaying antitumor activity and affecting the activity of calf thymus DNA topoisomerase 1I) 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 parenat compound (IDs0=0.001 !Ltmol/mL), and stimulated also the formafon of calf thymus topoisomerase II mediated pSP65 DNA cleavage in vitro at the concentration of 3 [aM. Being analogous to 9-hydroxyellipticine (wluch is an antitumor alkaloid), this novel indolo[2,3-b] quinoline derivative can be regarded as a novel potential antitumor agent.