Leo Hardegger

 

PhD Student

Location:

HCI G-304

Phone:

+41-1-633 4172

e-mail:

Leo Hardegger

Education

2003-2007:

BSc and MSc Study in Chemistry at ETH Zürich

2007:

Master thesis with Prof. F. Diederich at ETH Zürich

2008:

Internship at Novartis Institutes for BioMedical Research Inc., Cambridge, MA

since 2008:

Graduate Student with F. Diederich, ETH Zürich

2010:

Four-months exchange at F. Hoffmann-La Roche AG, Basel

Design and Synthesis of Protein Kinase B-Inhibitors


Protein kinase B (PKB/Akt) is a downstream protein in the phosphoinositol 3-kinase (PI3K) pathway. Its overexpression is observed in ovarian, breast, prostate, and pancreatic cancer in which the PI3K pathway is disregulated. This makes PKB an attractive molecular target for cancer therapy. Using Moloc®, we designed a number of potential inhibitors and propose their synthesis.

Publications

C. Faeh, L. A. Hardegger, L. Baitsch, W. B. Schweizer, S. Meyer, D. Bur, F. Diederich, Org. Biomol. Chem. 2009, 7, 3947-3957. New organofluorine building blocks: inhibition of the malarial aspartic proteases plasmepsin II and IV by alicyclic α,α-difluoroketone hydrates.

C. Faeh, L. A. Hardegger, M.-O. Ebert, W. B. Schweizer, F. Diederich, Chem. Commun. 2010, 46, 67-69. Self-association based on orthogonal C=O...C=O interactions in the solid and liquid state.

C. Faeh, R. Mathys, L. A. Hardegger, S. Meyer, D. Bur, F. Diederich, Eur. J. Org. Chem. 2010, 4617-4629. Enantiomerically Pure and Highly Substituted Alicyclic α,α-Difluoro Ketones: Potential Inhibitors for Malarial Aspartic Proteases, the Plasmepsins.

L. A. Hardegger, B. Kuhn, B. Spinnler, L. Anselm, R. Ecabert, M. Stihle, B. Gsell, R. Thoma, J. Diez, J. Benz, J.-M. Plancher, G. Hartmann, D. W. Banner, W. Haap, F. Diederich, Angew. Chem. Int. Ed. 2011, 50, 314-318. Systematic Investigation of Halogen Bonding in Protein-Ligand Interactions.

Last update: Jan. 2011