| Literature DB >> 19839622 |
Yang Liu1, Eleanor Peacey, John Dickson, Christine P Donahue, Suxin Zheng, Gabriele Varani, Michael S Wolfe.
Abstract
A series of mitoxantrone (MTX) analogues have been designed, synthesized, and evaluated for binding to and stabilizing a stem-loop structure that serves as a splicing regulatory element in the pre-mRNA of tau, which is involved in Alzheimer's and other neurodegenerative diseases. Several compounds showed significantly improved binding activity relative to the original screening hit mitoxantrone. These findings establish essential structure-activity relationships to further optimize the activity of this promising class of compounds.Entities:
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Year: 2009 PMID: 19839622 PMCID: PMC3808193 DOI: 10.1021/jm9013407
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446