1385774-90-2Relevant academic research and scientific papers
Synthesis of conformationally constrained benzoylureas as BH3-mimetics
Brady, Ryan M.,Hatzis, Effie,Connor, Theresa,Street, Ian P.,Baell, Jonathan B.,Lessene, Guillaume
, p. 5230 - 5237 (2012/08/08)
The design of small molecules that mimic the BH3 domain and bind to Bcl-2 proteins has emerged as a promising approach to discovering novel anti-cancer therapeutics. We reveal the design and synthesis of conformationally constrained benzoylurea scaffolds as conformational probes. Central to helix mimicry, the intramolecular hydrogen bond in the benzoylurea plays a key role in the pre-organisation of the acyclic substrates for cyclisation via ring closing metathesis, providing efficient access to the constrained mimetics. The Royal Society of Chemistry 2012.
