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초록
A series of pyrazolylpyrimidine scaffold based Syk inhibitors were synthesized and evaluated for their biological activities and selectivity. Lead optimization efforts provided compounds with potent Syk inhibition in both enzymatic and TNF-a release assay. (C) 2015 Elsevier Ltd. All rights reserved.
키워드
Spleen tyrosine kinase; Pyrazolylpyrimidine; Syk inhibitors; Rheumatoid arthritis; Structure-activity relationship; SPLEEN TYROSINE KINASE; DISCOVERY; INFLAMMATION; ACTIVATION; TARGET
- 제목
- Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors
- 저자
- Choi, Jang-Sik; Hwang, Hae-jun; Kim, Se-Won; Lee, Byung Il; Lee, Jaekyoo; Song, Ho-Juhn; Koh, Jong Sung; Kim, Jung-Ho; Lee, Phil Ho
- 발행일
- 2015-10-15
- 유형
- Article
- 권
- 25
- 호
- 20
- 페이지
- 4441 ~ 4446