Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin.

Autor: Aubry C; Department of Chemistry, University of Leicester, Leicester LE1 7RH, UK. kin@le.ac.uk, Wilson AJ, Jenkins PR, Mahale S, Chaudhuri B, Maréchal JD, Sutcliffe MJ
Jazyk: angličtina
Zdroj: Organic & biomolecular chemistry [Org Biomol Chem] 2006 Mar 07; Vol. 4 (5), pp. 787-801. Date of Electronic Publication: 2006 Feb 01.
DOI: 10.1039/b518019h
Abstrakt: We present the design, synthesis, and biological activity of three classes of tryptamine derivatives, which are non-planar analogues of the toxic anti-cancer agent fascaplysin. We show these compounds to be selective inhibitors of CDK4 over CDK2, the most active compound has an IC50 for the inhibition of CDK4 of 6 microM.
Databáze: MEDLINE