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| Description
| - The aim of this project is to develop novel drug candidates for improvement of the chemotherapy of tumors and malignancies of the haematopoietic system. The project results from an already existing knowledge and experience. The original compounds which are subject of this examination are based on a new structural principle which warrants their suitable clinical parameters, in particular their synergistic action with other anticancer drugs acting on different principles and, a comparative durability against multilple drug resistence (MDR). It concerns preclinical investigation of the 2nd generation of the so-called acyclic nucleoside phosphonates, namely N6-substituted derivatives of 2,6-diaminopurine with prospective antineoplastic activity, and their congeners. Additional activities of these compouds encompass intiviral and immunomodulatory activity. The project involves design, synthesis, biochemical (mode of action) and biological evaluation of selected drug candidates. (en)
- Cílem projektu je vývoj potenciálních léčiv pro zvýšení účinnosti chemotherapie neoplasií (nádorů, leukemií). Projekt vychází z existujících rozsáhlých poznatků a zkušenosti výzkumného týmu, týkajících se nového typu látek, objevených na UOCHB a vychází z předpokladu jejich synergických účinků s jinými léky působícími na odlišných mechanistických základech a na snížené pravděpodobnosti vzniku mnohočetné lékové resistence. Zahrnuje preklinický výzkum skupiny originálních látek vybraných na základě strukturně aktivitního studia, tzv. druhé generace fosfonátů acyklických nukleosidů, především látek ze skupiny N6-substituovaných derivátů 2,6-diaminopurinu s různým postranním řetězcem, u jejichž zástupců již byla nalezena význačná cytostatická aktivita. Látky mají i jiné významné účinky, především protivirový a imunostimulační. Obsahem projektu jsou návrhy struktury a syntéza nových látek, jejich biochemické studium (mechanismus účinku) a prověření biologických účinků in vitro i in vivo.
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| Title
| - Acyclic nucleoside phosponates with antineoplastic activity (en)
- Acyklické nukleosidfosfonáty s antineoplastickým účinkem
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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
| - antineoplastic;antileukemic;antitumor;cytostatic;nucleotide analogs;drug design;medicinal chemistr;antimetabolites;mechanisms;transplantable (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...okUkonceniPodpory
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| http://linked.open...okZahajeniPodpory
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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.../cep/vedlejsiObor
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| http://linked.open...jektu+dodavatelem
| - A series of promising antivirals was discovered; these open ring acyclic nucleoside phosphonates are derivatives of 2,4-diaminopyrimidine substituted with 6-phosphonoalkoxy group. (en)
- Byla objevena nová skupina významných antivirotik; jde o acyklické nukleosidfosfonáty s otevřeným kruhem. Jsou to deriváty 2,4-diaminopyrimidinu substituované 6-fosfono-alkoxyskupinou. (cs)
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| http://linked.open...tniCyklusProjektu
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| http://linked.open.../cep/klicoveSlovo
| - drug design
- mechanisms
- antitumor
- nucleotide analogs
- antileukemic
- antimetabolites
- antineoplastic
- cytostatic
- medicinal chemistr
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| is http://linked.open...vavai/riv/projekt
of | - Synthesis of 9-alkyl and 9-heteroalkyl substituted 2-amino-6-guanidinopurines and their influence on the NO-production in macrophages
- Synthesis and immunobiological activity of base substituted 2-amino-3-(purin-9-yl)propanoic acid derivatives
- Sonogashira cross-coupling in the synthesis of acyclic nucleoside phosphonates: preparation of 6-[(phosphonomethoxy)alkynyl]- and 6-[(phosphonomethoxy)alkyl]pyrimidines
- Novel acyclic nucleoside phosphonate analogues with potent anti-hepatitis B virus activities
- Involvement of adenosine A1 receptors in upregulation of nitric oxide by acyclic nucleotide analogues
- The substrate activity of (S)-9-[3-hydroxy-(2-phosphonomethoxy)propyl]adenine diphosphate toward DNA polymerases alpha, delta and epsilon
- Synthesis and antiviral activity of 2,4-diamino-5-cyano-6-[2-(phosphonomethoxy)ethoxy]pyrimidine and related compounds
- 6-Guanidinopurine nucleosides and their analogues.
- 6-[2-(Phosphonomethoxy)alkoxy]pyrimidines with antiviral activity.
- Evaluation of nucleoside phosphonates and their analogs and prodrugs for inhibition of orthopoxvirus replication.
- New 2-alkynyl derivatives of the acyclic nucleoside 9-(2,3-dihydroxypropyl)adenine and their 6-guanidinopurine counterparts as potential effectors of adenosine receptors.
- Interaction of phosphates of the acyclic nucleoside phosphonates with nucleoside diphosphate kinase from yeast and bovine liver
- Pronounced in vitro and in vivo antiretroviral activity of 5-substituted 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy] pyrimidines
- Towards the mechanism of trimeric purine nucleoside phosphorylases: Stopped-flow studies of binding of multisubstrate analogue inhibitor - 2-amino-9-[2-(phosphonomethoxy)ethyl]-6-sulfanylpurine
- Synthesis and cytostatic activity of N -[2-(phosphonomethoxy)alkyl]derivatives of N 6 -substituted adenines, 2,6-diaminopurines and related compounds.
- PMEDAP and its N 6 -substituted derivatives: genotoxic effect and apoptosis in vitro conditions.
- Solution structures of binary and ternary metal ion complexes of 9-(5-phosphonopentyl)adenine (3'-deoxa-PEEA). A nucleotide analogue related ti the antivirally active 9-[2-(phosphonomethoxy)ethyl]adenine (PMEA).
- Synthetic approaches to 'opened-ring' acyclic nucleoside phosphonates - novel type of antivirals.
- Tenofovir diphosphate is a poor substrate and a weak inhibitor of rat DNA polymerases .alfa., .delta., and .epsilon.
- Synthesis of optically active N 6 -alkyl derivatives of (R)-3-(adenin-9-yl)-2-hydroxypropanoic acid and related compounds.
- Synthesis of base substituted 2-hydroxy-3-(purin-9-yl)-propanoic acids and 4-(purin-9-yl)-3-butenoic acids.
- An efficient synthesis of cytostatic mono and bis-alkynylpyrimidine derivatives by the Sonogashira cross-coupling reactions of 2,4-diamino-6-iodopyrimidine and 2-amino-4,6-dichloropyrimidine
- Antiretroviral enantiomeric nucleotide analogs
- Synthesis of N9- and N7-[2-hydroxy-3-(phosphonomethoxy)-propyl] derivatives of N6-substituted adenines, 2,6-diaminopurines and related compounds
- 6-[2-(Phosphonomethoxy)alkoxy]-2,4-diaminopyrimidines: A new class of acyclic pyrimidine nucleoside phosphonates with antiviral activity
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| is http://linked.open...vavai/cep/projekt
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