Abstract by Prof. Dr. Mathias Christmann

The Chemistry and Biology of Englerin A

Sven Hahn, Tobias Seitz, Lea Radtke, Matthieu Willot, Mathias Christmann Although successful in many types of cancer, chemotherapy has shown at best moderate effectiveness in the treatment of renal cell carcinoma (RCC). Thus, the identification of novel inhibitors of kidney cancer signaling pathways remains highly desirable. A focused screening for specific inhibitors of renal cancer cell lines at the NCI led to the discovery of the guaiane sesquiterpenoid englerin A. [1] In 2009, our research group established the previously unknown absolute configuration of englerin A by total synthesis. [2] In subsequent work, we initiated intensive structureactivity investigations that resulted in the identification or more potent analogues. [3] Most recently, our ongoing collaborative studies have culminated in the identification of TRPC4 and TRPC5 Ca ²⁺ channels as a potential target. [4]

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[1] R. Ratnayake, D. Covell, TT Ransom, KR Gustafson, J. A Beutler, Org. Lett. 2009, 11, 57.
[2] M. Willot, L. Radtke, D. Könning, R. Fröhlich, VH Gessner, C. Strohmann, M. Christmann, Angew. Chem. Int. Ed. 2009, 48, 9105.
[3] L. Radtke, M. Willot, H. Sun, S. Ziegler, S. Sauerland, C. Strohmann, R. Fröhlich, P. habenberger, H. Waldmann, M. Christmann, Angew. Chem. Int. Ed. 2011, 50, 3998.
[4] Y. Akbulut, HJ Gaunt, K. Muraki, MJ Ludlow, MS Amer, A. Bruns, NS Vasudev, L. Radtke, M. Willot, S. Hahn, T. Seitz, S. Ziegler, M. Christmann , DJ Beech, H. Waldmann, Angew. Chem. Int. Ed. 2015, 54, 3787.

Curriculum Vitae of Prof. Dr. Mathias Christmann

* October 17, 1972 since 2013 - Professor (W3), Freie Universität Berlin, Germany
2008?2013 - Associate Professor (W2), Technische Universität Dortmund University, Germany
2003?2007 - Habilitation candidate, RWTH Aachen, Germany
2001?2002 - Postdoctoral Associate at the University of Minnesota, Minneapolis, MN, USA
Research Interests: Synthetic chemistry, Natural products synthesis, Organocatalysis and Sustainable Chemistry Awards: Carl Duisberg Memorial Prize (2013), Dechema Young Scientist Award for Natural Products Research (2012), Docent Fellowhip of the Fonds der Chemischen Industrie (2009), Liebig Fellowship of the Fonds der Chemischen Industrie (2003)