期刊
MEDCHEMCOMM
卷 4, 期 7, 页码 1085-1092出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3md00061c
关键词
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资金
- National Institutes of Health [RO1HL079207, PO1HL103455-02]
- Institute for Transfusion Medicine
- Hemophilia Center of Western Pennsylvania
- NIGMS CMLD initiative [P50GM067082]
- Boehringer Ingelheim Pharmaceuticals, Inc.
(1SR,4RS)-3,3-Dimethyl-1,2,3,4-tetrahydro-1,4-(epiminomethano)naphthalenes were synthesized in 2-3 steps from commercially available materials and assessed for specificity and effectiveness across a range of Nox isoforms. The N-pentyl and N-methylenethiophene substituted analogs 11g and 11h emerged as selective Nox2 inhibitors with cellular IC50 values of 20 and 32 mu M, respectively.
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