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Syntheses and biological activities of potent bombesin receptor antagonists.
Several inhibitors were able to recognize the bombesin receptor on rat pancreatic acini and antagonized bombsin stimulated amylase secretion in the nanomolar range and to inhibit [3H] thymidine incorporation in 3T3 cells with the same potency. Expand
Comparative Study of In Vitro and In Vivo Activities of Bombesin Pseudopeptide Analogs Modified on the C-Terminal Dipeptide Fragment
The results of this study showed that replacing the peptide bond between the two last amino acid residues in bombesin by mimicking the transition state analog resulted in in vitro and in vivo potentBombesin receptor antagonists. Expand
JMV641: A potent bombesin receptor antagonist that inhibits Swiss 3T3 cell proliferation
This compound was highly potent to dose-dependently inhibit binding of 125I-GRP to Swiss 3T3 cells and can inhibit bombesin-induced AP-1 regulated genes that are nuclear messengers mediating the actions of signal transduction pathways stimulated by growth factors. Expand
A synthetic glycine-extended bombesin analogue interacts with the GRP/bombesin receptor.
This study has tested the biological behaviour of a synthetic analogue of the glycine-extended bombesin (para-hydroxy-phenyl-propionyl-Gln-Trp-Ala-Val-Gly-His-Leu-Met- Gly-OH or JMV-1458) on various in vitro models and showed that this synthetic glycine/bombesin analogue induces its biological activities via the classical GRP/Bombesin receptor. Expand
Synthesis and biological evaluation of bombesin constrained analogues.
Analogues of bombesin which incorporate dipeptide or turn mimetics have been synthesized. One of them (compound 11) containing a seven-membered lactam ring revealed a good affinity for GRP/BNExpand
Synthesis of chiral urethane N-alkoxycarbonyl tetramic acids from urethane N-carboxyanhydrides (UNCAs)
Abstract The synthesis of chiral N-protected tetramic acid derivatives which are important precursors of β-hydroxy γ-amino acid under mild conditions is described. Reaction ofExpand
Syntheses and biological activities of bombesin analogs modified in the C-terminal dipeptide part
Summary Bombesin receptor antagonists are possible therapeutic agents due to their ability to act as inhibitors of cellular proliferation. On the basis of our hypothesis on the mechanism of action ofExpand
Synthesis of chiral N-protected amino acid esters by the use of UNCAs
An easy synthesis of N-protected amino acid esters, including tert-butyl esters, is described by the use of urethane N-protected carboxyanhydrides (UNCAs). Treating UNCAs with tert-butanol in theExpand
Synthesis and biological evaluation of C‐terminal hydroxamide analogues of bombesin
Interestingly, compound 1 behaved as a potent agonist in stimulating amylase secretion from rat pancreatic acini and is able to stimulate thymidine accumulation in 3T3 cells, while compound 2 was able to potently antagonize bombesin‐stimulated amyl enzyme secretion. Expand