BET

RWTH Technology

Highly Efficient and Selective Inhibitors Targeting BET Bromodomains

Challenge

BET proteins are important because they regulate both normal transcription processes as well as the transcription of oncogenes such as c-myc and Bcl-2 in various types of cancer. An efficient and selective inhibition of the BET proteins is therefore of great importance for cancer therapies. Various compounds, including benzenesulfonamide derivates are known to possess this property. However, there is a great desire for further, more selective inhibitors.

Solution

The use of sulfoximine, sulfondiimide and sulfonimidamide derivatives allows to generate novel molecules with a stereogenic sulfur atom. The utilization of this chirality provides new, highly effective and selective BET inhibitors.

Advantages

Novel BET inhibitors bearing a stereocenter
Chirality is the key to high efficacy and selectivity

Status

International patent application pending and German patent application pending
Proof of concept and ongoing research

RWTH Aachen University is looking for partners for patent exploitation.

Further details

Chiral Analogues of PFI-1 as BET Inhibitors and Their Functional Role in Myeloid Maligncies
B. Altenburg, M. Frings, J.-H. Schöbel, J. Goßen, K. Pannen, K. Vanderliek, G. Rossetti, S. Koschmieder, N. Chatain, C. Bolm, ACS Med. Chem. Lett. 2020, here.