Jump to main content
Jump to site search
Access to RSC content Close the message box

Continue to access RSC content when you are not at your institution. Follow our step-by-step guide.


Issue 27, 2012
Previous Article Next Article

Synthesis of conformationally constrained benzoylureas as BH3-mimetics

Author affiliations

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.

Graphical abstract: Synthesis of conformationally constrained benzoylureas as BH3-mimetics

Back to tab navigation

Supplementary files

Article information


Submitted
26 Mar 2012
Accepted
14 May 2012
First published
15 May 2012

Org. Biomol. Chem., 2012,10, 5230-5237
Article type
Paper

Synthesis of conformationally constrained benzoylureas as BH3-mimetics

R. M. Brady, E. Hatzis, T. Connor, I. P. Street, J. B. Baell and G. Lessene, Org. Biomol. Chem., 2012, 10, 5230
DOI: 10.1039/C2OB25618E

Social activity

Search articles by author

Spotlight

Advertisements