Identification of novel SAR properties of the Jak2 small molecule inhibitor G6: significance of the para-hydroxyl orientation |
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Authors: | Baskin Rebekah Gali Meghanath Park Sung O Zhao Zhizhuang Joe Keseru György M Bisht Kirpal S Sayeski Peter P |
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Institution: | Department of Physiology and Functional Genomics, University of Florida, Gainesville, FL, USA. |
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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. |
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