Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 10, Issue 27, Pages 5230-5237Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2ob25618e
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Funding
- National Health and Medical Research Council
- Leukaemia and Lymphoma Society
- Cancer Council Victoria
- Leukaemia Foundation
- Australian Cancer Research Foundation
- Australian Postgraduate Award
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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.
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