Naslov
New 6-substituted pyrimidine derivatives

Autori
Raić-Malić, Silvana ; Gazivoda, Tatjana ; Krištafor, Svjetlana ; Ametamey, Simon M.

Broj patenta
WO/2011/036505

Godina
2011

Datum patenta
31.03.2011

Nositelj prava
Sveučilište u Zagrebu, Zagreb ; Zurich, Hrvatska

Sažetak
The essence of the Invention comprises of the development of pluripotent pyrimidine derivatives. Pluripotent in this context means the property of compounds to be used and applied for different purposes. Thus, the compounds according to the subject Invention represent a new class of specific PET tracers that could provide a better insight into a tumor biology and monitoring, detection of relapse, monitoring of antitumor therapy efficiency. Furthermore, since the molecular imaging by PET allows tumor detection in its early stage (in size of only several mm), the more efficient application of this technique in combination with new selective PET tracers consequently reduces mortality caused by cancer. The informations that PET method provides are invaluable in staging, therapy planning, and therapeutic monitoring of cancer, and as such, are critical to succesful treatment and long-term cure of cancer. Moreover, several pyrimidine derivatives demonstrated cytostatic activities and could be used as anticancer agents. The new specifically halogenated pyrimidine nucleoside analogs that mimic the natural substrates, labeled with positron-emitting radioisotope, are incorporated into DNA and thus indicate the uncontrolled reproduction of tumor cells and changes caused by tumor growth. In a desirable design of the Invention, the pyrimidine derivatives are specifically fluorinated and labeled with the radioisotope 18F. Additinally, [18F]fluorinated with selective antiviral activity could also be used to localize HCMV infections, which is the main cause of death in patients after organ, especially bone marrow transplantations. The new nucleoside analogs as fraudulent substrates for HSV-1 TK, labeled with positron-emitting isotope 18F, give better insight to the field of gene therapy and the application of PET method in cancer treatment. Generally, the development of a non-invasive cell proliferation monitoring system using the specific PET tracers described in the subject Invention will contribute to a better quality of life of cancer patients, as well as to broadening the fundamental knowledge in the field of suicide gene therapy and PET technology.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

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