Potent small molecule inhibitors of spleen tyrosine kinase (Syk)
Potent small molecule inhibitors of spleen tyrosine kinase (Syk)
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DOI：
10.1016/s0960-894x(03)00658-9
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发表时间：
2003-09-15
影响因子：
2.7
通讯作者：
Bamborough, P
中科院分区：
文献类型：
--
作者：
Lai, JYQ;Cox, PJ;Bamborough, P
已经鉴定了一系列羟吲哚类化合物，其证明抑制Syk和IgE/Fc ε RI的生物素化底物的磷酸化触发嗜碱性细胞脱粒。讨论了磺胺31（IC 50 =5 nM，EC 50 = 1400 nM）周围SAR的研究。当极性表面积降低至< 110埃时，代表磺酰胺系列的适度细胞活性被克服（2），导致酰胺32的鉴定（IC 50 = 145 nM，EC 50 = 100 nM）。(C)2003年由爱思唯尔有限公司出版
A series of oxindoles demonstrating inhibition of the pbosphorylation of biotinylated substrates of Syk and IgE/FcepsilonRI triggered basophil cell degranulation has been identified. A study of the SAR around sulfonamide 31 (IC50=5 nM, EC50= 1400 nM) is discussed. The modest cellular activity representative of the sulfonamide series was overcome when the Polar surface Area was lowered to < 110 Angstrom(2), leading to the identification of amide 32 (IC50= 145 nM, EC50= 100 nM). (C) 2003 Published by Elsevier Ltd.