a, The total synthesis of the natural products YM-254890 (1) and FR900359 (2). b, Structures of two reduced analogues, YM-385780 (3) and YM-385781 (4), in which N-Me-Dha is replaced with either N-MeAla or N-Me-D-Ala. c, Structures of backbone-modified YM-254890 analogues (compounds 29–33) in which three N-methylated amide bonds and two ester bonds, respectively, are changed into amide bonds. d, Structures of YM-254890 analogues with modifications in the β-HyLeu moieties (compounds 34–38). DMF, N,N-dimethylformamide; TFA, trifluoroacetic acid.