Address115 avanenue Lacassagne, 69130 LyonFrance
Medicinal chemistry; Screening collections; FBDD; PPI; epigenetic targets
Natural by Design™: Edelris has pioneered for the past decade the design and synthesis of innovative, Natural Product-like small molecules (Keymical Collections™), aiming at the discovery of biorelevant chemical starting points towards hit and lead discovery.
Collaborations outside COST
European Lead Factory (http://www.imi.europa.eu/content/european-lead-factory)
Short description of ongoing research projects
- Epigenetic target (2014-2015): Hit optimization program leading to low nanomolar inhibitors
- Epigenetic target (2015): Design and synthesis of new inhibitors
- PPI inhibitors (2015): Design and synthesis of alpha helix mimetics
- “Total Synthesis of Bengamides B and E” F. Kinder, S. Wattanasin, R. W. Versace, K. W. Bair, J. Bontempo, M. A. Green, Y. J. Lu, H. Rao Marepalli, P. E. Phillips, D. Roche, L.D. Tran, R. Wang, L. Waykole, D. D. Xu, S. Zabludoff, J. Org. Chem. 2001, 66, 2118-2122.
- “ 1,4-Diazepane-2-ones as Novel Inhibitors of LFA-1” Sompong Wattanasin, Rainer Albert, C. Ehrhardt, D. Roche, M. Sabio, U. Hommel, K. Welzenbach, G. Weitz-Schmidt, Biorg. & Med. Chem. Lett. 2003, 13, 499-502.
- "Discovery and structure-guided drug design of inhibitors of 11.beta.-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold“. Lepifre, Franck; Christmann-Franck, Serge; Roche, Didier; Leriche, Caroline; Carniato, Denis; Charon, Christine; Bozec, Sophie; Doare, Liliane; Schmidlin, Fabien; Lecomte, Marc; Valeur, Eric. Bioorg. Med. Chem. Lett. 2009, 19(13), 3682-3685
- "First synthesis and biological properties of macrolactam analogs derived from natural product macrolide (-)-A26771B” Canova S, Lépine R, Thys A, Baron A, Roche D. Bioorg. Med. Chem. Lett. 2011, 21(16), 4768-72
- "Derivatives of macrocyclic natural product Branimycin” patent WO2015028095A1
Other activities of potential interest to others
Drug conjugates; Middle size rings & Macrocycles