The College of Education for Pure Sciences at the University of Basrah in the Department of Chemistry discussed a master’s thesis on (Preparation and study of the biological activity of coumarin derivatives)
The message presented by the researcher (Ayat Adel Ashour) included:
Compounds of benzopyrones, including coumarin, called benzo-α-pyrone, are found in nature in many plants, have many derivatives, have many benefits, and are characterized by their biological effectiveness. Therefore, the main goal was to prepare heterogeneous derivatives of coumarin using ultrasound waves, compare them with the traditional method (reflux distillation), and study their effectiveness. .
First: Preparation of the compound 7-Hydroxy-4-Methyl-2H-Chromen-2-one, its trade name - Methyl umbelliferone 4-, from the reaction of resorcinol with ethyl acetoacetate in sulfuric acid as a solvent. It is a basic compound for preparing derivatives, and four types of heterocyclic compounds were prepared from it. .
First class:-
Preparation of triazolothiadiazole derivatives of coumarin in three steps, where the coumarin ester is prepared and the hydrazide is converted using hydrazine, which was used to prepare triazolothiadiazole.
The second category: -
Preparation of Schiff bases from the hydrazide compound of coumarin by reacting it with some aldehydes.
The third category: -
Preparation of thiazolidinone derivatives of coumarin from bases prepared from hydrazide with thioglycolic acid.
Fourth category: -
Preparation of coumarin carbothiamide derivative from coumarin hydrazide with phenyl isothiocyanate.
The coumarin carbothiamide derivative was then reacted with sodium hydroxide to prepare the triazole derivative.
All the prepared compounds were characterized by diagnostic methods such as IR, 1H-NMR, 13C-NMR, and mass spectrometry.
Several studies were also conducted on the prepared compounds, where they studied their effectiveness against breast cancer type MCF-7 and calculated their IC50 value, as they gave high biological effectiveness in fighting cancer cells. The molecular docking of the prepared compounds on breast cancer proteins CDK4 was studied, and toxicity was studied using an international program, where the study gave Results showing the non-toxicity of the prepared compounds.
