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	Syntéza C-5 substituovaných derivátů HPMPC (Cidofoviru) Krečmerová, Marcela ; Holý, Antonín The series of N4-alkyl derivatives of (S)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-ethylcytosine was prepared from the corresponding 5-ethyl-4-methoxypyrimidin-2-(1H )-one intermediates by the action of primary amines. Sonogashira coupling was used for the preparation of 5-ethynyl HPMPC. Detailed record
	Pyrimidinové 1-[2-(fosfonomethoxy)propyl] deriváty: Jejich synthésy a využití jako potenciální inhibitory thymidinfosforylásy (PD-ECGF) z SD-lymfomu Pomeisl, Karel ; Votruba, Ivan ; Holý, Antonín ; Pohl, Radek In this study a novel method of transformation of HOCH2 group to FCH2 was successfully applied to the preparation of fluorine-containing pyrimidine 1-[3-fluoro-2-(phosphonomethoxy)-propyl] derivatives (FPMP compounds). The key displacement of hydroxy group with fluorine in better avalaible (S)- and (R)- 1-[3-hydroxy-2-(phosphonomethoxy)-propyl] derivatives (HPMP compounds) was performed using perfluorobutane-1-sulphonyl fluoride in the presence of DBU. Detailed record
	Acyklické nukleosid fosfonáty a inhibice lidské telomerázy Hájek, Miroslav ; Matulová, Naděžda ; Votruba, Ivan ; Holý, Antonín ; Tloušťová, Eva Diphosphates of acyclic nucleoside phosphonates were evaluated for their ability to inhibit human telomerase. Detailed record
	Design a syntéza 5,6-disubstituovaných uracilových derivátů jako účinných inhibitorů thymidinfosforylasy Nencka, Radim ; Votruba, Ivan ; Hřebabecký, Hubert ; Tloušťová, Eva ; Horská, Květoslava ; Masojídková, Milena ; Holý, Antonín We report on a series of novel 5,6-disubstituted uracils with significant inhibitory activity against human and Escherichia coli thymidine phosphorylases. Detailed record
	Syntéza nových racemických konformačně omezených karbocyklických nukleosidů Šála, Michal ; Hřebabecký, Hubert ; Masojídková, Milena ; Holý, Antonín Novel racemic conformationally locked nucleosides, derived from bicyclo[2.2.1]heptene or heptane, were prepared and tested for their biological activity. Detailed record
	N6-methyl-AMP-hydrolasa aktivuje N6-substituované purinové ANPs Schinkmanová, Markéta ; Votruba, Ivan ; Holý, Antonín Identification and characterization of a new enzyme, N6-methyl-AMP aminohydrolase, that is responsible for the conversion of N6-cyclopropyl-PMEDAP to biologically active PMEG. Detailed record
	Acyklické bis-fosfonátové nukleosidy - nová analoga ANP Vrbovská, Silvie ; Holý, Antonín As a part of the systematic SAR study in ANP series (many of ANP derivatives posses significant antiviral and cytostatic activity), we intended to study the behavior of ANP analogues bearing in the molecule two phosphonate residues. Detailed record
	Tricyklické etheno analogy purinů odvozené od 2-amino-6-chlorpurinu Hořejší, Kateřina ; Pohl, Radek ; Holý, Antonín A series of new linear and angular tricyclic etheno-bridged derivatives was synthesized from 2-amino-6-chloropurine and regioselectivity of the cyclization reaction was studied. Detailed record
	Syntéza a vlastnosti chirálních acyklických nukleosid bisfosfonátů s otevřeným kruhem Doláková, Petra ; Masojídková, Milena ; Holý, Antonín A new type of acyclic nucleoside phosphonates (ANP) is derived from 2,4-diamino-6-hydroxypyrimidine. These 6-[2-(phosphonomethoxy)ethoxy]pyrimidine derivatives significantly inhibit replication of retroviruses and herpesviruses in cell cultures. This novel subclass of pyrimidine ANPs can be considered as analogues of 2,6-diaminopurine with an open imidazole ring in the purine moiety. Detailed record
	Syntéza N4-substituovaných derivátů 1-[(S)-3-hydroxy-2-(phosphonomethoxy)propyl]cytosinu (HPMPC, Cidofovir, Vistide) Chalupová, Šárka ; Holý, Antonín 1-[(S)-3-hydroxy-2-(phosphonomethoxy)propyl]cytosine (HPMPC, Cidofovir) has a broad activity spectrum against DNA viruses. As the systemic drug VireadTM is used for treatment of cytomegalovirus retinitis in AIDS patients. Based on this unique profile of HPMPC we have investigated the effect of the substitution of the amino function at the position 4 upon the antiviral activity. Detailed record

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