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Synthesis of amides - Organic chemistry

R.; Lober, S.; Hubner, H.; Gmeiner, P., Click chemistry on solid phase: parallel synthesis of -benzyltriazole carboxamides as super-potent G-protein coupled receptor ligands.

Bombesin receptor ligand analogues have been used in clinical studies however the high potency of agonists brings up challenges requiring synthesis with high specific radioactivity in order to exclude pharmacological effects. Antagonists even though they do not internalize have shown improved imaging capabilities. Given recent achievements in the design of antagonists and experience with SST analogues demonstrating advantages of antagonists, the future development will most likely move in the direction of bombesin antagonists.

Modular Synthesis of ChiraClick Ligands: A Library of P-Chirogenic Phosphines.

Click Chemistry Publications - Scripps Research Institute

295. Shetty D, Jeong JM, Ju CH, Kim YJ, Lee JY, Lee YS. . Synthesis and evaluation of macrocyclic amino acid derivatives for tumor imaging by gallium-68 positron emission tomography. 2010;18:7338-47

305. Fontes A, Prata MIM, Geraldes C, Andre JP. Ga(III) chelates of amphiphilic DOTA-based ligands: synthetic route and in vitro and in vivo studies. 2011;38:363-70

PDF Downloads : Oriental Journal of Chemistry

138. Yim CB, van der Wildt B, Dijkgraaf I, Joosten L, Eek A, Versluis C. . Spacer effects on in vivo properties of DOTA-conjugated dimeric [Tyr3]octreotate peptides synthesized by a "Cu(I)-click" and "sulfo-click" ligation method. 2011;12:750-60

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