299439-16-0Relevant articles and documents
Scaffold hopping via ANCHOR.QUERY: β-lactams as potent p53-MDM2 antagonists
Shaabani,Neochoritis,Twarda-Clapa,Musielak,Holak,D?mling
supporting information, p. 1046 - 1052 (2017/07/12)
Using the pharmacophore-based virtual screening platform ANCHOR.QUERY, we morphed our recently described Ugi-4CR scaffold towards a β-lactam scaffold with potent p53-MDM2 antagonizing activities. 2D-HSQC and FP measurements confirm potent MDM2 binding. Molecular modeling studies were used to understand the observed SAR in the β-lactam series.