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Chemistry

Synthesis of simaomicin-a to enable derivatization

A method to synthesize the natural compound simaomicin-a could help the development of analogs for use in cancer. Simaomicin-a, a polycyclic xanthone, is derived from an actinomycete and was previously shown to synergize with the DNA-damaging agent bleomycin to kill cancer cells. In vitro, simaomicin-a was synthesized using palladium-mediated dehydrogenative coupling of two aryl rings to create the key biaryl linkage in the molecule. In multiple human cancer cell lines, the synthetic simaomicin-a inhibited growth with nanomolar IC50 values comparable to those of natural simaomicin-a. Next steps include studies to understand the mechanism of simaomicin-a.

SciBX 6(37); doi:10.1038/scibx.2013.1039
Published online Sept. 26, 2013

Unpatented; available for licensing

Wang, Y. et al. Angew. Chem. Int. Ed.; published online Aug. 22, 2013;
doi:10.1002/anie.201304812
Contact: Joseph M. Ready,
The University of Texas Southwestern Medical Center, Dallas, Texas
e-mail:

joseph.ready@utsouthwestern.edu