1,2,3,4-Tetrahydropyrimidine-clubbed quinoline hybrid: Radiolabeling, Biodistribution and Imaging

Abstract

Cancer represents a broad category encompassing various diseases that can impact any area of the body. It is also referred to as malignant tumors or neoplasms. Aiming to diagnose tumors, a promising monastrol analogue (1b) methyl 4-(2-hydroxyquinolin-3-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate, was designed via structural modification of monastrol, and synthesized in good yield. This compound was in vitro evaluated via MTT assay and revealed potent antitumor effects on a panel of cancer cell lines namely; HepG-2, HCT-116, MCF-7, and PC3 against standard 5-fluorouracil. The target 1b was radiolabeled with iodine-131 by a direct electrophilic substitution reaction. It was found that 131I-1b has a high radiolabeling yield (96.40 ± 2.00%), stability, solid tumor uptake, and Target/Non-target ratio (T/NT) ratio (5 ± 0.03 at 30 min. post-injection) compared with many new tracers which have been developed in recent years. This study encourages the possible use of this tracer as a potential imaging and/or therapeutic agent for cancer.