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Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.
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.
Afiliación
  • Choi JS; Department of Chemistry, Kangwon National University, Chuncheon 200-701, Republic of Korea; Oscotec Inc., 694-1 Sampyeong-dong, Bundang-gu, Seongnam-si, Gyeonggi-do 463-400, Republic of Korea.
  • Hwang HJ; Oscotec Inc., 694-1 Sampyeong-dong, Bundang-gu, Seongnam-si, Gyeonggi-do 463-400, Republic of Korea.
  • Kim SW; Oscotec Inc., 694-1 Sampyeong-dong, Bundang-gu, Seongnam-si, Gyeonggi-do 463-400, Republic of Korea.
  • Lee BI; Biomolecular Function Research Branch, Division of Convergence Technology, Research Institute, National Cancer Center, Goyang, Gyeonggi 410-769, Republic of Korea.
  • Lee J; Genosco, 767C Concord Avenue, 2nd Floor, Cambridge, MA 02138, USA.
  • Song HJ; Genosco, 767C Concord Avenue, 2nd Floor, Cambridge, MA 02138, USA.
  • Koh JS; Genosco, 767C Concord Avenue, 2nd Floor, Cambridge, MA 02138, USA.
  • Kim JH; Oscotec Inc., 694-1 Sampyeong-dong, Bundang-gu, Seongnam-si, Gyeonggi-do 463-400, Republic of Korea. Electronic address: jhkim@oscotec.com.
  • Lee PH; Department of Chemistry, Kangwon National University, Chuncheon 200-701, Republic of Korea. Electronic address: phlee@kangwon.ac.kr.
Bioorg Med Chem Lett ; 25(20): 4441-6, 2015 Oct 15.
Article en En | MEDLINE | ID: mdl-26384287
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-α release assay.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Pirimidinas / Proteínas Tirosina Quinasas / Péptidos y Proteínas de Señalización Intracelular / Inhibidores de Proteínas Quinasas Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Pirimidinas / Proteínas Tirosina Quinasas / Péptidos y Proteínas de Señalización Intracelular / Inhibidores de Proteínas Quinasas Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article