Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 3, Pages 1402-1407Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.12.042
Keywords
Jak2 tyrosine kinase; G6; Small molecule inhibitor; Stilbenoid; SAR
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Funding
- National Institutes of Health [R01-HL67277]
- University of Florida
- University of Florida/Moffitt Cancer Center Collaborative Initiative
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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. (C) 2011 Elsevier Ltd. All rights reserved.
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