No abstract

No abstract

A structure-activity relationship (SAR) study of bastadin 6 (1), a brominated tyrosine-derived metabolite from Indonesian marine sponge having a potent anti-angiogenic activity, was executed. The syntheses and their biological evaluation of the oxime-modified analogues and bromine-modified analogues revealed that both the oxime moieties and bromine atoms in bastadin 6 (1) play an important role to show the potent and selective anti-proliferative activity against human umbilical vein endothelial cells (HUVECs).

Efficient Total Synthesis of Bastadin 6, an anti-Angiogenic Brominated Tyrosine-Derived Metabolite from Marine Sponge. -(KOTOKU, N.; TSUJITA, H.; HIRAMATSU, A.; MORI, C.; KOIZUMI, N.; KOBAYASHI*, M.; Tetrahedron 61 (2005) 30, 7211-7218; Grad. Sch. Pharm. Sci., Osaka Univ., Suita, Osaka 565, Japan; Eng.) -Nuesgen 46-208

Addition reactionsAddition reactions O 0060 1,4-Addition Reaction of Ethyl Bromodifluoroacetate to Michael Acceptors in the Presence of Copper Powder Improvement of the Reaction Using TMEDA as an Additive. -Reaction of ethyl bromodifluoroacetate (II) with a variety of Michael acceptors of type (I) or (IV) is considerably improved by the addition of TMEDA. -(SATO, K.; NAKAZATO, S.; ENKO, H.; TSUJITA, H.; FUJITA, K.; YAMAMOTO, T.; OMOTE, M.; ANDO, A.; KUMADAKI*, I.; J. Fluorine Chem. 121 (2003) 1, 105-107; Fac. Pharm. Sci., Setsunan Univ., Hirakata, Osaka 573-01, Japan; Eng.) -M. Bohle 32-033