Structure-Based Design of New KSP-Eg5 Inhibitors Assisted by a Targeted Multicomponent Reaction (pages 1471–1480)
Carlos Carbajales, Dr. Miguel Ángel Prado, Dr. Hugo Gutiérrez-de-Terán, Ángel Cores, Dr. Jhonny Azuaje, Dr. Silvia Novio, Prof. María Jesús Nuñez, Dr. Belén Fernández-García, Prof. Eddy Sotelo, Prof. Xerardo García-Mera, Prof. Pedro Sánchez-Lazo, Prof. Manuel Freire-Garabal and Prof. Alberto Coelho
Article first published online: 18 JUN 2014 | DOI: 10.1002/cbic.201402089
A focused inhibitor library: In silico design and the four-component Ugi reaction were combined to produce a library of low-micromolar-range inhibitors of kinesin spindle protein (KSP) with antiproliferative activity. The most active compounds were synthesized with high efficiency by taking advantage of the multicomponent reactions.