Doing the methylene shuffle - Further insights into the inhibition of mitotic kinesin Eg5 with S-trityl l-cysteine

► Quantification of the binding interactions of STLC in complex with Eg5. ► SAR study describing new analogues of STLC with modification to the trityl system. ► Novel analogues with IC50 values <100 nM against Eg5. ► SAR of P-glycoprotein induced resistance for this class of compounds.