Xanthocillin derivatives, which show thrombopoietin receptor agonist activity, were synthesized through our developed method. Bioassay data suggest the importance of alkene geometry, the presence of substituents at the benzene ring that support hydrophobic character, and the moderate size of the molecule. One of the two isonitrile group of the natural product appears to be dispensable.

Receptor binding activity X 0280Structure-Activity Relationships of Xanthocillin Derivatives as Thrombopoietin Receptor Agonist. -Syntheses and bioassay are given. The results of the latter suggest the importance of the alkene geometry, the presence of hydrophobic substituents at the benzene rings, and the moderate molecule size. All active compounds [cf. (I) and (II)] show inhibition of cell proliferation at high concentration. -(YAMAGUCHI, T.; MIYAKE, Y.; MIYAMURA, A.; ISHIWATA, N.; TATSUTA*, K.; J. Antibiot. 59 (2006) 11, 729-734; Dep. Chem., Sch. Sci. Eng., Waseda Univ., Shinjuku, Tokyo 169, Japan; Eng.) -H. Haber