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Org Biomol Chem. 2012 Apr 21;10(15):2928-33. doi: 10.1039/c2ob07125h. Epub 2012 Mar 7.

Relaxation of the rigid backbone of an oligoamide-foldamer-based α-helix mimetic: identification of potent Bcl-xL inhibitors.

Author information

1
Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 N Pine St, Baltimore, MD 21201, USA.

Abstract

By conducting a structure-activity relationship study of the backbone of a series of oligoamide-foldamer-based α-helix mimetics of the Bak BH3 helix, we have identified especially potent inhibitors of Bcl-x(L). The most potent compound has a K(i) value of 94 nM in vitro, and single-digit micromolar IC(50) values against the proliferation of several Bcl-x(L)-overexpressing cancer cell lines.

PMID:
22395339
DOI:
10.1039/c2ob07125h
[Indexed for MEDLINE]

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