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Org Biomol Chem. 2012 Jul 21;10(27):5230-7. doi: 10.1039/c2ob25618e. Epub 2012 May 30.

Synthesis of conformationally constrained benzoylureas as BH3-mimetics.

Author information

1
Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia.

Abstract

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.

PMID:
22648632
DOI:
10.1039/c2ob25618e
[Indexed for MEDLINE]

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