Preclinical evaluation of new GnRH-I receptor radionuclide therapy with Lu-peptide tracer.

The purpose of this study was to develop preclinical evaluation of a novel radiolabeled gonadotropin-releasing hormone (GnRH) receptor targeting peptide for prostate cancer therapy. The new antiproliferative agent of GnRH-I analogue was developed on the basis of the D-Trp -GnRH-I scaffold, and in vivo pharmacokinetics and receptor binding affinity were enhanced by the substitution of Gly-NHNH for Gly-NH at position 10 in D-Trp -GnRH-I. To evaluate Lu-DOTA-triptorelin-hydrazide as radionuclide therapy of tumor, the quality control tests and preclinical stage assessment were carried out.

Preparation of four 1,4-dihydropyridine derivatives (DHPs) labeled with carbon-14.

The importance of DHPs compounds and the need for examining the mechanism of their effect, mandated us to synthesize a number of carbon-14 labeled 1,4-dihydropyridine derivatives for pharmacological studies. Simple preparation and suitable radiochemical yield were advantages of this preparation.

Synthesis of 2 carbon-14 analogue of thioflavanones.

Thioflavanones are prevalent heterocyclic structural units in pharmaceutical and biologically active compound (Scheme ). In this paper, the synthesis of 2-phenylthiochroman-4-ones and 2-phenyl-4H-1-benzothiopyran-4-one labeled with carboxyl-14 is demonstrated.

Synthesis of (2-mercaptoacetyl)-L-[2- C]tryptophan as a selective metallo-β-lactamase inhibitor via [2- C]indole based on chiral pool strategy.

Metallo-beta-lactamase enzymes make bacteria resistant to a broad range of commonly used beta-lactam antibiotics. Several thiol derivatives of L-amino acids have been shown their inhibitory effects against the metallo-β-lactamase IMP-1. In this study, (2-mercaptoacetyl)-L-tryptophan as a new inhibitor of metallo-β-lactamases labeled with carbon-14 in the 2-position of the indole ring was prepared from [2- C]indole as a key synthetic intermediate based on chiral pool strategy.

Preparation of 1-fluoro-4-methyl-9H-[carbonyl-(14) C]thioxanthen-9-one and amine derivatives.

9H-Thioxanthen-9-ones are an important class of compound and are a common heterocyclic scaffold in biologically active and medicinally significant compounds. In this paper the synthesis of 1-fluoro-4-methyl-9H-thioxanthen-9-one and some amine derivatives labeled with carboxyl-14 is described.

Synthesis of 2-(methylsulfonyl)-5-(4-(methylsulfonyl) phenyl)-4-phenyl-1H-[5-(14)C]imidazole, a selective COX-2 inhibitor, via asymmetrical benzoins.

4,5-Diarylimidazoles labeled with carbon-14 in the 5-position of the imidazole ring were prepared as a part of three-step sequence from 2-hydroxy-1-(4-(methylthio)phenyl)-2-phenyl[1-(14) C]ethanone as a key synthetic intermediate which has been synthesized from potassium [(14) C]cyanide.

Synthesis of a series of carbon-14 labeled tetrahydropyrido[4,3-d]pyrimidin-4(3H)-ones.

A series of tetrahydropyrido[4,3-d]pyrimidin-4(3H)-ones labeled with carbon-14 in the 2-position of pyrimidinone moiety were prepared as part of a 3-step sequence from benz[amidino-(14) C]amidine hydrochloride as a key synthetic intermediate.

Synthesis of carbon-14 analogue of 1,5 diaryl-5-[14C]-1,2,3-triazoles.

Two 1,2,3-triazole anticonvulsants, 1-(4-methylsulfone-phenyl)-5-(4-methyl-phenyl)-1,2,3-triazole and 1-(4-methylsulfone-phenyl)-5-phenyl-1,2,3-triazole, both labeled with carbon-14 in the 5-position were prepared from para-tolunitrile-[cyano-14C] and benzonitrile-[cyano-14C], respectively.