Research Output per year
Novel small molecule inhibitors of heat shock protein 90 (Hsp90) were discovered with the help of a fragment based drug discovery approach (FBDD) and subsequent optimization with a combination of structure guided design, parallel synthesis and application of medicinal chemistry principles. These efforts led to the identification of compound 18 (NMS-E973), which displayed significant efficacy in a human ovarian A2780 xenograft tumor model, with a mechanism of action confirmed in vivo by typical modulation of known Hsp90 client proteins, and with a favorable pharmacokinetic and safety profile.
- Anti-cancer agents
- Fragment based drug discovery
- Tumor cell proliferation inhibition
Corrigendum to “Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90)” [Bioorg. Med. Chem. 21 (2013) 7047–7063]Brasca, M. G., Mantegani, S., Amboldi, N., Bindi, S., Caronni, D., Casale, E., Ceccarelli, W., Colombo, N., De Ponti, A., Donati, D., Ermoli, A., Fachin, G., Felder, E. R., Ferguson, R. D., Fiorelli, C., Guanci, M., Isacchi, A., Pesenti, E., Polucci, P., Riceputi, L. & 4 others, , 1 Jan 2014, In : Bioorganic & Medicinal Chemistry. 22, 1, p. 662 1 p.
Research output: Contribution to journal › Article