Radioiodination of 2,3-dimethyl-4H-furo[3,2-c]coumarin and biological evaluation in solid tumor bearing mice

Abstract

Compound 2,3-dimethyl-4H-furo[3,2-c]coumarin is a coumarin derivative that could be labeled with 125I. The process of labeling was started using 1 mg of the compound, 50 µg CAT oxidizing agent, 30 min as reaction time at pH with a yield about 95%. The 125I-coumarin derivative was stable for about 48 h. Radiochemical purity of the labeled compound was performed by electrophoresis and HPLC. The labeled compound was separated with purity about 95%. Tumor transplantation to produce a solid tumor in the right leg of albino mice was made by intramuscular injection of 2×106 EAC (Ehrlish acittes carcinoma cells). Biodistribution study of 125I-coumarin derivative revealed that the uptake in tumor bearing leg was over 5% at 1 h and 4 h post-injection. This uptake encourages the use of 123I-coumarin derivative in imaging of tumor sites.

Furo[3,2-c]coumarins carrying carbon substituents at C-2 and/or C-3. Isolation, biological activity, synthesis and reaction mechanisms

“…The results (5% uptake) supported the potential use of this heterocycle as a probe for imaging of tumor sites. 46…”

Thiazole Ring—A Biologically Active Scaffold

“…Among the three most active compounds, the highest was achieved for compound 75b (IC 50 8.17 ± 1.89 µM and 3.15 ± 1.68 µM), being more potent against the gastric carcinoma (MGC803) cell lines. This is an indication that not only the nature but also the position of the substituent affects the anticancer activity.Mohammed et al[115], based on the literature survey regarding the antitumor activity of coumarin compounds[116,117] as well as thiazole derivatives[118], combined these two moieties in one molecule and synthesized the potassium salt of 5-(4-chlorophenyl)-2-[(7hydroxycoumarin-3-ylethylidene)acetylhydrazine]-1,3-thiazole (76a) and 5-(4-chlorophenyl)-2-[(8-hydroxycoumarin-3-ylethylidene)acetylhydrazine]-1,3-thiazole (76b) with the aim to investigate in vivo their antitumor activity (Figure29). Compounds were tested for their effect on caspase-3 and Bax (BCL-2 associated protein) in Ehrlich ascites carcinoma (EAC) and in the liver.…”

In vivo Biochemical Evaluation of Some Synthesize Thiazole Derivatives Containing Coumarin Moiety as Antioxidant and Antitumor Agents

“…Coumarin compounds possessing anti-bacterial [6,7], Antifungal [8][9][10], anticoagulant [11], antituberculosis [12], anti-inflammatory [11], antitumor [13,14], anti-human immunodeficiency virus (HIV) activities [15]. Its substitution effectively influences the biological activities of the synthesized coumarin derivatives.…”