Cs. Swindell et al., CHARACTERIZATION OF THE TAXOL STRUCTURE-ACTIVITY PROFILE FOR THE LOCUS OF THE A-RING SIDE-CHAIN, Bioorganic & medicinal chemistry letters, 4(12), 1994, pp. 1531-1536
Two series of taxol analogs with various N-acyl groups on 3'-phenyliso
serine and isoserine A-ring side chains, respectively, were prepared,
and their microtubule assembly activities and cytotoxicities toward J7
74.2 cells were evaluated. Biological activities were adversely affect
ed by the structural modifications investigated, although the 3'-pheny
lisoserine series was significantly more active than the isoserine ser
ies.