Extensive SAR studies on the unselective BRS3 agonist, [H-D-Phe6,beta-Ala11,Phe13,Nle14]-bombesin-(6-14)-nonapeptide amide, have highlighted structural features important for BRS3 activity and have provided guidance as to the design of selective agonists. A radically modified heptapeptide agonist, maintaining only the Trp-Ala moiety of the parent [H-D-Phe6,betaAla11,Phe13,Nle14]-peptide amide, and with a very different carboxyl terminal region, has been produced which was potent at BRS3 and essentially had no NMB or GRP receptor activity. Its structure is Ac-Phe-Trp-Ala-His(tauBzl)-Nip-Gly-Arg-NH2.
Three new quassinoids and four new quassinoid glycosides were isolated from water-soluble fraction of methanol extract of seeds of Brucea javanica (L.) Merr, known as “Ya-dan-zi” in Chinese folklore and their structures were determined by spectral and chemical means. Yadanziosides F, I, J, and L were demonstrated to have antileukemic activity.
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