Recent advances in the medicinal chemistry of taxoids with novel beta-amino acid side chains

beta-Amino acids have been recognized as an important class of compounds in the design and synthesis of potential pharmaceutical drugs and also for th e study of enzymatic reaction mechanisms. Among the beta-amino acid family, isoserines (alpha-hydroxy-beta-amino acids) are probably the most importan t members because many of them are potent enzyme inhibitors and they also s erve as essential building blocks for biologically and medicinally importan t molecules such as Taxol(R). Taxol(R) (paclitaxel) and Taxotere(R)(docetax el) are currently considered to be the most important drugs in cancer chemo therapy. This review describes recent advances in the chemistry of isoserin es and taxoid anticancer agents at the biomedical interface including (i) t he development of highly efficient method for the synthesis of isoserine si de chains of taxoids and (ii) the synthesis and structure-activity relation ship (SAR) study of taxoids featuring discovery and development of the "sec ond generation" taxoid anticancer agents that possess exceptional activitie s against drug-resistant cancer cells.