Marcela Krečmerová

Summary

Affiliation: Institute of Organic Chemistry and Biochemistry
Country: Czech Republic

Publications

  1. ncbi request reprint Antiviral activity of triazine analogues of 1-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]cytosine (cidofovir) and related compounds
    Marcela Krečmerová
    Gilead Sciences and IOCB Research Centre, Centre for New Antivirals and Antineoplastics IOCB, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic
    J Med Chem 50:1069-77. 2007
  2. ncbi request reprint Alpha anomer of 5-aza-2'-deoxycytidine down-regulates hTERT mRNA expression in human leukemia HL-60 cells
    Miroslav Hájek
    Gilead Sciences Research Center, Institute of Organic Chemistry and Biochemistry v v i, AS CR, 166 10 Prague 6, Czech Republic
    Biochem Pharmacol 75:965-72. 2008
  3. doi request reprint 9-[2-(R)-(Phosphonomethoxy)propyl]-2,6-diaminopurine (R)-PMPDAP and its prodrugs: optimized preparation, including identification of by-products formed, and antiviral evaluation in vitro
    Marcela Krečmerová
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v v i Flemingovo nám 2, 16610 Prague 6, Czech Republic
    Bioorg Med Chem 21:1199-208. 2013
  4. doi request reprint Synthesis of purine N9-[2-hydroxy-3-O-(phosphonomethoxy)propyl] derivatives and their side-chain modified analogs as potential antimalarial agents
    Marcela Krečmerová
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v v i, Flemingovo nam 2, CZ 166 10 Prague 6, Czech Republic
    Bioorg Med Chem 20:1222-30. 2012
  5. doi request reprint 5-azacytosine compounds in medicinal chemistry: current stage and future perspectives
    Marcela Krečmerová
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v v i, Flemingovo nam 2, 16610 Prague 6, Czech Republic
    Future Med Chem 4:991-1005. 2012
  6. doi request reprint Synthesis of ester prodrugs of 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-2,6-diaminopurine (HPMPDAP) as anti-poxvirus agents
    Marcela Krečmerová
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic
    J Med Chem 53:6825-37. 2010
  7. doi request reprint Acyclic nucleoside phosphonates with 5-azacytosine base moiety substituted in C-6 position
    Marcela Krečmerová
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, vvi, Gilead Sciences and IOCB Research Centre, Flemingovo nam 2, CZ 166 10, Prague 6, Czech Republic
    Bioorg Med Chem 18:387-95. 2010
  8. ncbi request reprint Ester prodrugs of cyclic 1-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-azacytosine: synthesis and antiviral activity
    Marcela Krečmerová
    Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic
    J Med Chem 50:5765-72. 2007
  9. doi request reprint New prodrugs of Adefovir and Cidofovir
    Tomas Tichy
    Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Prague 166 10, Czech Republic
    Bioorg Med Chem 19:3527-39. 2011
  10. doi request reprint Synthesis and antiviral activities of hexadecyloxypropyl prodrugs of acyclic nucleoside phosphonates containing guanine or hypoxanthine and a (S)-HPMP or PEE acyclic moiety
    Tomas Tichy
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v v i, Flemingovo nam 2, Prague 166 10, Czech Republic
    Eur J Med Chem 55:307-14. 2012

Collaborators

Detail Information

Publications15

  1. ncbi request reprint Antiviral activity of triazine analogues of 1-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]cytosine (cidofovir) and related compounds
    Marcela Krečmerová
    Gilead Sciences and IOCB Research Centre, Centre for New Antivirals and Antineoplastics IOCB, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic
    J Med Chem 50:1069-77. 2007
    ..Decomposition of 1 in alkaline solutions resulted in products 17 and 18. While the N-formylguanidine derivative 17 proved active, the carbamyolguanidine derivative 18 was devoid of antiviral activity...
  2. ncbi request reprint Alpha anomer of 5-aza-2'-deoxycytidine down-regulates hTERT mRNA expression in human leukemia HL-60 cells
    Miroslav Hájek
    Gilead Sciences Research Center, Institute of Organic Chemistry and Biochemistry v v i, AS CR, 166 10 Prague 6, Czech Republic
    Biochem Pharmacol 75:965-72. 2008
    ..Although the primary task of hypomethylating agents in anticancer therapy lies in reactivation of silenced tumour-suppressor genes, the inhibition of hTERT expression might also be a fruitful clinical effect of this approach...
  3. doi request reprint 9-[2-(R)-(Phosphonomethoxy)propyl]-2,6-diaminopurine (R)-PMPDAP and its prodrugs: optimized preparation, including identification of by-products formed, and antiviral evaluation in vitro
    Marcela Krečmerová
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v v i Flemingovo nám 2, 16610 Prague 6, Czech Republic
    Bioorg Med Chem 21:1199-208. 2013
    ..Compared to the parent molecule, the amidate prodrug was 10-fold less active against FIV in cell culture, whereas the alkoxyalkyl ester prodrug was 200-fold more potent in inhibiting FIV replication in vitro...
  4. doi request reprint Synthesis of purine N9-[2-hydroxy-3-O-(phosphonomethoxy)propyl] derivatives and their side-chain modified analogs as potential antimalarial agents
    Marcela Krečmerová
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v v i, Flemingovo nam 2, CZ 166 10 Prague 6, Czech Republic
    Bioorg Med Chem 20:1222-30. 2012
    ..This suggests that the covalent attachment of a second group to the ANPs mimicking pyrophosphate and occupying its binding pocket could increase the affinity for these enzymes...
  5. doi request reprint 5-azacytosine compounds in medicinal chemistry: current stage and future perspectives
    Marcela Krečmerová
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v v i, Flemingovo nam 2, 16610 Prague 6, Czech Republic
    Future Med Chem 4:991-1005. 2012
    ..Considering the potential pharmaceutical applications, 5-azacytosine and 5,6-dihydro-5-azacytosine appear to be so far the most effective cytosine mimics for the design of novel antiviral and anti-tumor drug candidates...
  6. doi request reprint Synthesis of ester prodrugs of 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-2,6-diaminopurine (HPMPDAP) as anti-poxvirus agents
    Marcela Krečmerová
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic
    J Med Chem 53:6825-37. 2010
    ....
  7. doi request reprint Acyclic nucleoside phosphonates with 5-azacytosine base moiety substituted in C-6 position
    Marcela Krečmerová
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, vvi, Gilead Sciences and IOCB Research Centre, Flemingovo nam 2, CZ 166 10, Prague 6, Czech Republic
    Bioorg Med Chem 18:387-95. 2010
    ..Surprisingly, N-3 isomer of 6-methyl-HPMP-5-azaC in the form of isopropyl ester revealed activity against RNA viruses (Sindbis virus)...
  8. ncbi request reprint Ester prodrugs of cyclic 1-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-azacytosine: synthesis and antiviral activity
    Marcela Krečmerová
    Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic
    J Med Chem 50:5765-72. 2007
    ..The relative configuration of the diastereoisomer trans-6 was determined using H,H-NOESY NMR...
  9. doi request reprint New prodrugs of Adefovir and Cidofovir
    Tomas Tichy
    Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Prague 166 10, Czech Republic
    Bioorg Med Chem 19:3527-39. 2011
    ..S)-HPMPC prodrugs exhibited anti-cytomegalovirus activities in the same range as the parent drug, whereas the anti-HSV and anti-VZV activities were one- to seven-fold lower than that of Cidofovir...
  10. doi request reprint Synthesis and antiviral activities of hexadecyloxypropyl prodrugs of acyclic nucleoside phosphonates containing guanine or hypoxanthine and a (S)-HPMP or PEE acyclic moiety
    Tomas Tichy
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v v i, Flemingovo nam 2, Prague 166 10, Czech Republic
    Eur J Med Chem 55:307-14. 2012
    ..Monoesters of (S)-HPMPG emerged as the most potent and selective derivatives against these DNA viruses. None of the compounds were inhibitory against RNA viruses and retroviruses...
  11. doi request reprint An enzymatic glycosylation of nucleoside analogues using β-galactosidase from Escherichia coli
    Jiří Blažek
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of Czech Republic, v v i, Flemingovo namesti 2, CZ 166 10 Prague 6, Czech Republic
    Bioorg Med Chem 20:3111-8. 2012
    ....
  12. doi request reprint Study of chemical stability of antivirally active 5-azacytosine acyclic nucleoside phosphonates using NMR spectroscopy
    Martin Dracinsky
    Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v v i, Flemingovo nam 2, CZ 166 10 Prague 6, Czech Republic
    Bioorg Med Chem 16:6778-82. 2008
    ..The reaction pathway of HPMP-5-azaC involves a formyl derivative formed by intramolecular transformylation reaction...
  13. doi request reprint Syntheses of 1-[2-(Phosphonomethoxy)Alkyl] thymine monophosphates and an evaluation of their inhibitory activity toward human thymidine phosphorylase
    Karel Pomeisl
    Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v v i, Prague, Czech Republic
    Nucleosides Nucleotides Nucleic Acids 31:159-71. 2012
    ..The highest inhibitory potency was found with (R)-FPMPTp 4c (K (i) (dT) = 4.09 ± 0.47 μM, K (i)(P(i)) = 2.13 ± 0.29 μM) and (R) 3-MeO-PMPTp 4d (K (i) (dT) = 5.78 ± 0.71 μM, K (i)(P(i)) = 2.71 ± 0.37 μM)...
  14. doi request reprint 8-Aza-7,9-dideazaxanthine acyclic nucleoside phosphonate inhibitors of thymidine phosphorylase
    David Mařák
    Institute of Organic Chemistry and Biochemistry, v v i, Gilead Sciences and IOCB Research Center, Academy of Sciences of the Czech Republic, Flemingovo nam 2, 166 10 Prague 6, Czech Republic
    Bioorg Med Chem Lett 21:652-4. 2011
    ..The IC(50) values ranged from 3.5 to 27μM...
  15. ncbi request reprint Nucleotide analogues with immunobiological properties: 9-[2-Hydroxy-3-(phosphonomethoxy)propyl]-adenine (HPMPA), -2,6-diaminopurine (HPMPDAP), and their N6-substituted derivatives
    Petr Potmesil
    Institute of Experimental Medicine, Academy of Sciences of the Czech Republic, Centre for New Antivirals and Antineoplastics, Videnska 1083, 142 20 Prague 4, Czech Republic
    Eur J Pharmacol 540:191-9. 2006
    ..The immunomodulatory effects were found to be at least in part dependent on P1 purinoreceptors, and mediated by transcriptional factor nuclear factor-kappaB...