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Bioorg Med Chem Lett. 2012 Feb 1;22(3):1402-7. doi: 10.1016/j.bmcl.2011.12.042. Epub 2011 Dec 21.

Identification of novel SAR properties of the Jak2 small molecule inhibitor G6: significance of the para-hydroxyl orientation.

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1
Department of Physiology and Functional Genomics, University of Florida, Gainesville, FL, USA.

Abstract

In this study, we analyzed the structure-activity relationship properties of the small molecule Jak2 inhibitor G6. We synthesized a set of derivatives containing the native para-hydroxyl structure or an alternative meta-hydroxyl structure and examined their Jak2 inhibitory properties. We found that the para-hydroxyl derivative known as NB15 had excellent Jak2 inhibitory properties in silico, in vitro, and ex vivo when compared with meta-hydroxyl derivatives. These results indicate that NB15 is a potent derivative of the Jak2 inhibitor G6, and that maintaining the para-hydroxyl orientation of G6 is critical for its Jak2 inhibitory potential.

PMID:
22227213
PMCID:
PMC3267892
DOI:
10.1016/j.bmcl.2011.12.042
[Indexed for MEDLINE]
Free PMC Article
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