化学
部分
全合成
蛋白酶体
酰胺
立体化学
效力
机制(生物学)
组合化学
生物化学
体外
认识论
哲学
作者
Songnian Lin,Zhi-Qiang Yang,Benjamin H. Kwok,Michael A. Koldobskiy,Craig M. Crews,Samuel J. Danishefsky
摘要
A full account of the total syntheses of proteasome inhibitors TMC-95A and -B is provided. A key feature of the syntheses involved installation of a cis-propenylamide moiety by a thermal rearrangement of an α-silylallyl amide. The scope and mechanism of the enamide-forming reaction are discussed. Also provided are some preliminary results from SAR studies. It was found that simplified analogues can retain the full potency of proteasome inhibition.
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