The discovery of BMS-275183: an orally efficacious novel taxane

Abstract The evolution of 2 , a C-4-methylcarbonate analogue of paclitaxel with minimal oral bioavailability and oral efficacy, into its C-3′- t -butyl-3′- N - t -butyloxycarbonyl analogue ( 15i ), a novel taxane with oral efficacy in preclinical models that is comparable to iv administered paclitaxel, is described.