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Cancer; Mycobacterium

DNA; topoisomerase II (TOP2)

In vitro studies identified analogs of the natural product chartreusin that could serve as lead compounds to help treat cancer or mycobacterial infection. Chartreusin binds DNA and inhibits TOP2. Chemical synthesis, biosynthesis, SAR and in vitro testing of chartreusin analogs identified several lead compounds that inhibited proliferation of human colon cancer, melanoma and/or chronic myeloid leukemia (CML) cell lines at low micromolar to high nanomolar GI50 values. Another lead compound inhibited growth of M. vaccae at a low micromolar minimum inhibitory concentration. Planned work includes optimizing the lead compounds to treat cancer or mycobacterial infection.

SciBX 6(45); doi:10.1038/scibx.2013.1301
Published online Nov. 21, 2013

Patented by the Hans Knoell Institute; available for partnering and licensing

Ueberschaar, N. et al. J. Am. Chem. Soc.; published online Oct. 21, 2013;
Contact: Christian Hertweck, Hans Knoell Institute, Jena, Germany