Identification of tertiary sulfonamides as RORc inverse agonists

Identification of tertiary sulfonamides as RORc inverse agonists
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DOI:
10.1016/j.bmcl.2014.03.038
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发表时间:
2014-05-01
影响因子:
2.7
通讯作者:
Wong, Harvey
Wong, Harvey
中科院分区:
医学4区
文献类型:
--
作者:
Fauber, Benjamin P.;Rene, Olivier;Wong, Harvey

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Screening a nuclear receptor compound subset in a RORc biochemical binding assay revealed a benzylic tertiary sulfonamide hit. Herein, we describe the identification of compounds with improved RORc biochemical inverse agonist activity and cellular potencies. These improved compounds also possessed appreciable selectivity for RORc over other nuclear receptors. (C) 2014 Elsevier Ltd. All rights reserved.