Title: 

N-substituted tacrine compounds, how they are made and their applications. 

Protection status: 

Patent No Pat.235351 

Subject: 

The invention relates to the obtained innovative compounds belonging to tricyclic systems with potential use in cancer treatment with coexisting Alzheimer’s disease. The synthesized compounds, due to the presence of a known pharmacophore group of a therapeutic substance used in Alzheimer’s disease, show affinity for acetylcholinesterase belonging to the cholinergic system of the central nervous system. The mechanism involving stimulation of this system is the primary therapeutic target in the treatment of this disease. In addition, the structure of the invention is in the form of a chemical hybrid, the second fragment of which, due to its pleated arrangement and previous literature reports on the relationship between structure and action of therapeutic substances, indicates the possibility of intercalation into DNA strand chains. Thus, it will be responsible for cell-destructive activity. 

Benefits: 

“Multifunctional drugs” – the substances obtained are multifunctional substances (potential anticancer drugs with a cognitive enhancement component) – one substance acted on several handle points. 

Stage of work: 

A series of 9 new biologically active substances were obtained, their chemical structure was determined, and basic biological tests were performed to confirm the assumed direction of action. Each of these substances was tested for action on enzymes and systems of the central nervous system, for each of these substances the effect on selected cancer cell lines was determined. 

Application: 

Production of preparations used in geriatrics and cancer treatment. 

Contact: 

@: jaroslaw.kowalewski@umed.lodz.pl, tel.: 797 604 075