Naslov
Synthesis, Biological Evaluations and 18F-Radiolabeling of C-6 Substituted Thymine Derivatives

Autori
Gazivoda, Tatjana ; Krištafor, Svjetlana ; Martić, Miljen ; Ametamey, Simon ; Scapozza, Leonardo ; Raić-Malić, Silvana

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
XXI. Hrvatski skup kemičara i kemijskih inženjera / Novak, Predrag - Trogir : Hrvatsko društvo kemijskih inženjera i tehnologa (HDKI), 2009, 101-101

ISBN
978-953-6894-38-3

Skup
XXI. Hrvatski skup kemičara i kemijskih inženjera

Mjesto i datum
Trogir, Hrvatska, 19.04.2009. - 22.04.2009

Vrsta sudjelovanja
Poster

Vrsta recenzije
Domaća recenzija

Ključne riječi
C-6 Substituted Thymine Derivatives; 18F-Radiolabeling; Positron Emission Tomography

Sažetak
The novel C-6 substituted pyrimidine derivatives were designed and synthesized by multistep synthetic strategy involving nucleophilic addition of lithiated 2, 4-dimethoxy-5, 6-dimethylpyrimidine to 1, 3-bis(benzyloxy)propan-2-one, radical deoxygenation, N-methylation and deprotection of methoxy and benzyl groups to give the 6-(1, 3-dihydroxyisobutyl)-1-methylthymine and its corresponding unsaturated structural congener. The target molecules, which were selectively phosphorylated by herpes simplex virus type-1 thymidine kinase (HSV-1 TK) and not by human TK, exhibited good binding affinities for viral TK and no cytotoxicities [1]. Thus, they fulfilled the necessary requirements for their application as tracer molecules for non-invasive TK imaging by positron emission tomography (PET). [1] Johayem A., Raić-Malić, S., Lazzati, K., Schubiger P.A., Scapozza, L., Ametamey, S., Chem. & Biodiv. 3 (2006) 274 ; Raić-Malić S., Johayem A., Ametamey S., Batinac S., De Clercq E., Folkers G., Scapozza L., 23 Nucleosides, Nucleotides & Nucleic Acids (2004) 1707.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

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