Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton’s tyrosine kinase (BTK) and Janus kinase 2 (JAK2)

[Display omitted] Four series of disubstituted carbazole-1-carboxamides were designed and synthesised as inhibitors of Bruton’s tyrosine kinase (BTK). 4,7- and 4,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of BTK, while 3,7- and 3,6-disubstituted carbazole-1-carboxa...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2015-10, Vol.25 (19), p.4265-4269
Hauptverfasser: Liu, Qingjie, Batt, Douglas G., Lippy, Jonathan S., Surti, Neha, Tebben, Andrew J., Muckelbauer, Jodi K., Chen, Lin, An, Yongmi, Chang, Chiehying, Pokross, Matt, Yang, Zheng, Wang, Haiqing, Burke, James R., Carter, Percy H., Tino, Joseph A.
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Sprache:eng
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Zusammenfassung:[Display omitted] Four series of disubstituted carbazole-1-carboxamides were designed and synthesised as inhibitors of Bruton’s tyrosine kinase (BTK). 4,7- and 4,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of BTK, while 3,7- and 3,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of Janus kinase 2 (JAK2).
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2015.07.102