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|Title:||Precursor-directed generation of indolocarbazoles with topoisomerase IIα inhibitory activity|
Guangxi University for Nationalities
Ocean University of China
Chinese Academy of Sciences
Qingdao National Laboratory for Marine Science and Technology
|Keywords:||Pharmacology, Toxicology and Pharmaceutics|
|Citation:||Marine Drugs. Vol.16, No.5 (2018)|
|Abstract:||© 2018 by the authors. One new indolocarbazole, 3-hydroxy-K252d (3), together with the recently reported 3-hydroxyholyrine A (1) and 3-N-acetyl-3-hydroxyholyrine A (2), were obtained by feeding a culture of the marine-derived Streptomyces strain OUCMDZ-3118 with 5-hydroxy-L-tryptophan. Their structures were elucidated on the basis of spectroscopic analysis. Compound 1 potently induced apoptosis of gastric cancer cells by inhibiting topoisomerase IIα enzyme activity and reducing the expression of antiapoptosis protein level. Compound 3 displayed moderate cytotoxicity against the A549 and MCF-7 cell lines with IC50 values of 1.2 ± 0.05 µM, 1.6 ± 0.09 µM, respectively.|
|Appears in Collections:||Scopus 2018|
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