Design, synthesis, and structure− affinity relationships of novel series of sialosides as CD22-specific inhibitors

HHM Abdu-Allah, T Tamanaka, J Yu…

文献索引：Abdu-Allah, Hajjaj H. M.; Tamanaka, Taichi; Yu, Jie; Zhuoyuan, Lu; Sadagopan, Magesh; Adachi, Takahiro; Tsubata, Takeshi; Kelm, Soerge; Ishida, Hideharu; Kiso, Makoto Journal of Medicinal Chemistry, 2008 , vol. 51, # 21 p. 6665 - 6681

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被引用次数: 21

摘要

Sialosides incorporating substituted amides or amines at 9-position of sialic acid moiety have been synthesized and evaluated as CD22 inhibitors. Several derivatives exhibited inhibitory potency in sub-to low micromolar range (eg, 8o, 9d, 9g, and 9k showed IC50 values 0.40, 0.47, 0.24, and 0.23 μM, respectively, for hCD22, while 8p, 8q, and 9f, showed IC50 values 1.70, 2.90, and 4.10 μM, respectively, for mCD22). The most significant result ...