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| Description
| - The aim of this project is to develop novel antivirals and/or cytostatics based on nucleoside, nucleotide and nucleobase structure, to determine their transport characteristics, metabolism and mechanism of action, under the conditions acceptable for preclinical phase of drug development. The project concerns five groups of modified compounds: (1) structural variation of our antiviral drug cidofovir (a drug highly efficient against poxviruses) at the N4 and/or C-5 position of the cytosine base; (2) side-chain modification of 2,4-diamino-;pyrimidine bearing a 3'-substituted 2'-(phosphonoalkoxy)propoxy group at the position C-6; (3) 6-C-substituted (hetaryl, hydroxyalkyl) purine nucleosides with potential cytostatic or anti-RNA viral activity; (4) hydrophilic (water-soluble) derivatives of covalent base-pair models connected by alkane, alkene or alkyne units with cytostatic potential and (5) carbocyclic analogs of substituted pyrimidine nucleosides with potential antiangiogenic activity. (en)
- Cílem projektu je vyvinout nová léčiva na bázi analogů nukleosidů, nukleotidů a nukleobazí pro terapii viro-vých chorob a nádorových onemocnění. Stanovit charakteristiky jejich transportu do buněk, jejich metabolické přeměny a mechanismus účinku, za podmínek použitelných pro preklinickou fázi vývoje. Program počítá s pěti základními skupinami sloučenin: (1) strukturní variace cidofoviru, našeho anti-DNA virového preparátu, vysoce účinného na poxviry, na heterocyklické bázi cytosinu v polohách N4 a C5; (2) modifikace postranního řetězce 2,4-diaminopyrimidinu s 3'-substituovanými 2'-(fosfonoalkoxy)propoxyskupinami v poloze 6; (3) nukleosidy 6-C-substituovaných (hetaryl, hydroxyalkyl)purinů s anti-RNA virovým nebo cytostatickým účinkem; (4) hydrofilní (vodorozpustné) deriváty kovalentních modelů párů bazí, spojených alkanovými, alkenovými či alkynovými můstky, s možnými účinky cytostatickými a (5) karbocyklické analogy subst. pyrimidinových nukleosidů s možným účinkem antiangiogenním.
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| Title
| - Novel antivirals and antineoplastics (en)
- Nová antivirotika a antineoplastika
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| skos:notation
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| http://linked.open...avai/cep/aktivita
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| http://linked.open...kovaStatniPodpora
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| http://linked.open...ep/celkoveNaklady
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| http://linked.open...datumDodatniDoRIV
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| http://linked.open...i/cep/druhSouteze
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| http://linked.open...ep/duvernostUdaju
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| http://linked.open.../cep/fazeProjektu
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| http://linked.open...ai/cep/hlavniObor
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| http://linked.open...hodnoceniProjektu
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| http://linked.open...vai/cep/kategorie
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| http://linked.open.../cep/klicovaSlova
| - cytistatics; antivirals; antileukemics; nucleosides; nucleotides; ANP; nucleobases; antiangiogenics; carbocyclic analogs; poxviruses; variola virus; bioterrorism; HCV; HBV; AIDS; medicinal chemistry; new drugs; purines; tissue cultures; resistent mutant (en)
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| http://linked.open...ep/partnetrHlavni
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| http://linked.open...inujicichPrijemcu
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| http://linked.open...cep/pocetPrijemcu
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| http://linked.open...ocetSpoluPrijemcu
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| http://linked.open.../pocetVysledkuRIV
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| http://linked.open...enychVysledkuVRIV
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| http://linked.open...lneniVMinulemRoce
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| http://linked.open.../prideleniPodpory
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| http://linked.open...iciPoslednihoRoku
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| http://linked.open...atUdajeProjZameru
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| http://linked.open.../vavai/cep/soutez
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| http://linked.open...usZobrazovaneFaze
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| http://linked.open...ai/cep/typPojektu
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| http://linked.open...ep/ukonceniReseni
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| http://linked.open.../cep/vedlejsiObor
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| http://linked.open...ep/zahajeniReseni
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| http://linked.open...jektu+dodavatelem
| - New highly active antivirals based on acyclic nucleoside phosphonates and their open-ring analogs were discovered and their metabolism and mechanism of action was proved. New type of nanomolar cytostatics was found based on 7-deazapurine nucleosides. (en)
- Byla objevena nová vysoce aktivní antivirotika na bázi acyklických nukleosid fosfonátů a jejich open-ring analogů a prostudován jejich metabolismus a mechanismus účinku. Byl objeven nový typ nanomolárních cytostatik na bázi 7-deazapurinových nukleosidů. (cs)
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| http://linked.open...tniCyklusProjektu
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| http://linked.open.../cep/klicoveSlovo
| - AIDS
- HCV
- antivirals
- nucleosides
- nucleotides
- purines
- tissue cultures
- ANP
- HBV
- antiangiogenics
- antileukemics
- bioterrorism
- carbocyclic analogs
- medicinal chemistry
- new drugs
- nucleobases
- poxviruses
- variola virus
- cytistatics
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| is http://linked.open...vavai/riv/projekt
of | - Alpha anomer of 5-aza-2'-deoxycytidine down-regulates hTERT mRNA expression in human leukemia HL-60 cells
- Synthesis, cytostatic and anti-HCV activity of 6-(N-substituted aminomethyl)-, 6-(O-substituted hydroxymethyl)- and 6-(S-substituted sulfanylmethyl)purine nucleosides
- Synthesis, cytostatic and antiviral activity of novel 6-[2-(dialkylamino)ethyl]-, 6-(2-alkoxyethyl)-, 6-[2-(alkylsulfanyl)ethyl]- and 6-[2-(dialkylamino)vinyl]purine nucleosides
- Hydroxymethylations of aryl halides by Pd-catalyzed cross-couplings with (benzoyloxy)methylzinc iodide - the scope and limitations of the reaction
- Synthesis of novel carbocyclic nucleoside analogues containing bicyclo[2.2.1]hept-2-ene-2-methanol
- Human N6-Methyl-AMP/dAMP aminohydrolase (abacavir 5’-monophosphate deaminase) is capable of metabolizing N6-substituted purine acyclic nucleoside phosphonates
- Synthesis of 6-(4,5-dihydrofuran-2-yl)- and 6-(tetrahydrofuran-2-yl)purine bases and nucleosides
- Synthesis of substituted 6-cyclopropylpurine bases and nucleosides by cross-coupling reactions or cyclopropanations
- Purine bases and nucleosides bearing functionalized C-subtituents in position 6. Synthesis and biological activities
- Synthesis of (purin-6-yl)acetates and their transformations
- New antiviral agent, 1-(S)-[3-hydroxy-(2-phosphonomethoxy)propyl]-5-azacytosin: esters and base modified derivatives
- Metalation of 6-halo-2,4-dimethoxypyrimidines as the key step for the synthesis of biologicaly active compounds
- Synthesis of N9-(3-fluoro-2-phosphonomethoxypropyl) (FPMP) derivatives of N6 substituted adenines and 2,6-diaminopurines
- Efficient synthesis of OPEN-RING, CLOSE-RING acyclic nucleoside phosphonates
- Facile syntheses of pyrimidine acyclic nucleoside phosphonates and their potential evaluation for biomedical applications
- Synthesis of acyclic nucleoside diphosphate mimics
- Study of chemical stability of antivirally active 5-azacytosine acyclic nucleoside phosphonate using NMR spectroscopy
- Nucleosides and nucleotides containing 8-aza-7,9-dideazaxanthine
- Synthesis of 8-C-substituted 2,6-diaminopurine acyclic nucleoside phosphonates by Negishi cross-couplin
- Study of chemical stability of antivirally active 5-azacytosine acyclic nucleoside phosphonates using NMR spectroscopy
- Cytostatic and Antiviral 6-Arylpurine Ribonucleosides IX: Synthesis and Evaluation of 6-Substituted 3-Deazapurine Ribonucleosides
- Synthesis of diverse 6-(1,2-disubstituted ethyl)purine bases and nucleosides via 6-(oxiran-2-yl)purines
- Intracellular metabolism of the new antiviral compound 1-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-azacytosine
- Enzymatic polymerization of phosphonate nucleosides
- Mechanism of antiviral drug resistance of vaccinia virus: Identification of residues in the viral DNA polymerase conferring differential resistance to anti-poxvirus drugs
- Synthesis of analogues of acyclic nucleoside diphosphates containing a (phosphonomethyl)phosphanyl moiety and studies of their phosphorylation
- Synthesis of novel carbocyclic nucleoside analogues derived from 7-oxabicyclo[2.2.1]heptane-2-methanol
- Synthesis of novel racemic carbocyclic nucleoside analogues derived from 4,8-dioxatricyclo[4.2.1.0 3,7]nonane-9-methanol and 4-oxatricyclo[4.3.1.0 3,7]decane-10-methanol, compounds with activity against Coxsackie viruses
- Cross-coupling Reactions of Halopurines with Aryl- and Alkyltrifluoroborates. The Scope and Limitations in the Synthesis of Modified Purines
- Inhibition of hypoxanthine-guanine phosphoribosyltransferase by acyclic nucleoside phosphonates: A new class of antimalarial therapeutics
- Synthesis of branched 9-[2-(2-phosphonoethoxy)ethyl]purines as a new class of acyclic nucleoside phosphonates which inhibit Plasmodium falciparum hypoxanthine-guanine-xanthine phosphoribosyltransferase
- Chiral analysis of anti-acquired immunodeficiency syndrome drug, 9-(R)-[2-(phosphonomethoxy)propyl]adenine (tenofovir), and related antiviral acyclic nucleoside phosphonates by CE using beta-CD as chiral selector
- Synthesis of (purin-6-yl)acetates and their transformations to 6-(2-hydroxyethyl)- and 6-(carbamoylmethyl)purines
- Use of Pd-catalyzed Suzuki-Miyaura coupling reaction in the rapid synthesis of 5-aryl-6-(phosphonomethoxy)uracils and evaluation of their inhibitory effect towards human thymidine phosphorylase
- Norbornane as the novel pseudoglycone moiety in nucleosides
- New carbocyclic nucleoside analogues built on a bicyclo[2.2.2]octane-2,2-dimethanol template
- 6-(Het)aryl-7-Deazapurine Ribonucleosides as Novel Potent Cytostatic Agents
- Synthesis of novel racemic carbocyclic nucleosides derived from 5,6-disubstituted norbornene
- Structural diversity of nucleoside phosphonic acids as a key factor in the discovery of potent inhibitors of rat T-cell lymphoma thymidine phosphorylase
- Distinct modulation of telomere length in two T-lymphoblastic leukemia cell lines by cytotoxic nucleoside phosphonates PMEG and PMEDAP
- Synthesis of guanidino analogues of PMPDAP and their immunobiological activity
- Purine P1 receptor-dependent immunostimulatory effects of antiviral acyclic analogues of adenine and 2,6-diaminopurine
- N6-methyl-AMP hydrolase activates N6-substituted purine ANPs
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