In light of the increasing interest in the syntheses of fluorocarbohydrates as well as in their radiolabelled analogues for use in positron emission tomography (PET), a two- step synthesis of 2-fluoro-2-deoxy-ß-D-allose (2-FDpA) has been developed. The present synthesis employed electrophilic fluorination of 3,4,6-tri-O-acetyl-D-glucal in anhydrous HF (aHF) solvent using F2 and AcOF and was more rapid and efficient than the existing synthesis of 2-deoxy-2-fluoro-D-allose, with a total synthesis time of approximately 45 min, and less laborious. The synthesis proved to be higly regio- and Stereosective, which is often hard to achieve from electrophilic fluorinations. The synthetic route to 2-FDßA was used to obtain the 18F-Iabelled analogue, 2-[18F]FDßA, for the first time with the anticipation that the labelled compound will be of use as a diagnostic agent for the detection and assessment of different tumours as well as for monitoring D-allose metabolism. The overall decay-corrected radiochemical yields (RCY) of the products resulting from radiofluorination of TAG in aHF with [18F]F2 and [18F]AcOF were 33 ±3% and 9 ±2%, respectively, with respect to [18FJF2. The RCY of 33 ±3% is the highest reported for direct fluorinations of TAG using [18FJF2 in any solvent. The radiochemical purities of 2-[18F]FDßA were 96 ±3% and 91 ±8% as determined by radio-HPLC and radio-TLC, respectively. Preliminary in vivo studies using normal rats showed significant differences between the uptake of 2-[18F]FDßA and 2-[18F]FDG, the most commonly used PET radiotracer for detection of various types of cancers. In addition, an animal study with a Polynoma Middle T mouse showed retention of 2-[18F]FDßA in the tumour. The 18F-Iabelling technique was also used as a mechanistic probe for the synthesis of 2-FDßA in the present study. / Thesis / Master of Science (MSc)

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Krūties piktybiniai navikai – viena svarbiausių sveikatos apsaugos problemų visame pasaulyje. Vėžiu ar kita piktybine liga sergantį pacientą turi nuolat stebėti gydytojas onkologas, o lygiagrečiai galima taikyti ir augalų terapiją, kadangi tai padidina chemoterapijos efektyvumą ir padeda sumažinti nepageidaujamą jos pašalinį poveikį. „Onkofit M“ receptūrą pasiūlė Prof. Dr. V. F. Korsun. Darbe aprašomas „Onkofit M“ preparatų (vaistažolių arbatos ir kietųjų kapsulių su sausaisiais augaliniais ekstraktais) technologijos kūrimas ir pateikti vaistinių augalinių žaliavų, įeinančių į “Onkofit M” sudėtį, aprašymai, farmakologiniai poveikiai, cheminės sudėtys, kurie pagrindžia pasirinkimą. Nustatyta, kad sausųjų augalinių ekstraktų mišinio technologinės savybės nepalankios kapsuliavimui, todėl jos suteiktos modeliuojant pagalbines medžiagas bei jų kiekius. Parinkta „Onkofit M“ kapsuliuojamos masės sudėtis. Teisingas mišinio sudėties parinkimas patvirtintas UAB „Aconitum“ – pagaminta eksperimentinė serija pilotiniam tyrimui. Patikrintas eksperimentinės serijos „Onkofit M“ kapsulių stabilumas. Parinkta placebo kapsuliuojamos masės sudėtis ir pagamintos pilotiniam tyrimui reikalingos placebo kapsulės. Paruoštas ir supakuotas į popierinius maišelius vaistažolių mišinys arbatai, vertintas jo stabilumas. / Malignant breast tumours – one of the most important health care issues in the world. A patient who is having a cancer must be constantly monitored by an oncologist and at the same type fitotherapy may be applied as well that can improve the efficiency of chemotherapy and reduce its side effects. The formula of “Onkofit M” has been introduced by V. F. Korsun. The development of the technology of “Onkofit M” preparations (herbal teas and solid capsules with dry extracts) description of herbal ingredients, pharmacological effects, chemical composition that validate the choice of certain components, are represented in this study. It has been identified that technological properties of dry plant extracts mixture are not suitable for capsulation; therefore they have been improved while varying types and amounts of additives. The proper composition of “Onkofit M” was selected and it was approved by UAB “Aconitum” – the experimental batch was manufactured for the pilot research. The stability of the experimental batch of “Onkofit M” capsules was tested. The composition of placebo capsules was determed and batch of such capsules was also manufactured for the pilot research. Herbal tea was prepared and packaged in paper bags; stability tests were performed as well.