Solid-phase synthesis of azidomethylene inhibitors targeting cysteine proteases

Organic Letters
Peng-Yu YangShao Q Yao

Abstract

An efficient strategy for the solid-phase synthesis of azidomethylene inhibitors targeting cysteine proteases is described. The method is highlighted by its compatibility with readily available building blocks, as well as its ability to accommodate different functional groups. A 249-member library has thus far been successfully synthesized, characterized, and screened against Caspase-1, -3 and -7.

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Citations

Feb 6, 2015·Chembiochem : a European Journal of Chemical Biology·Pengyu Yang, Kai Liu
May 14, 2009·Accounts of Chemical Research·Mahesh UttamchandaniShao Q Yao
Jul 5, 2008·Journal of Combinatorial Chemistry·Tracey PiraliArmando A Genazzani

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