Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 21, Pages 6042-6046Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.09.057
Keywords
ERK1/2; Substrate-specific inhibitor; Synthesis; SAR; Thiazolidine-2,4-dione; Rational design; Molecular modeling
Categories
Funding
- American Cancer Society [IRG-73-001-34]
- NIH [CA 10086]
- Virginia Commonwealth University
Ask authors/readers for more resources
A series of analogs of 3-(2-amino-ethyl)-5-(4-ethoxy-benzylidene)-thiazolidine-2,4-dione, a putative substrate-specific ERK1/2 inhibitor, were synthesized and biologically characterized in human leukemia U937 cells to de. ne its pharmacophore. It was discovered that shift of ethoxy substitution from the 4-to the 2-position on the phenyl ring significantly improved functional activities of inhibiting cell proliferation and inducing apoptosis. This may provide access to a new lead for developing ERK1/2 substrate-specific inhibitors. Published by Elsevier Ltd.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available