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1 180 (0,148s)

Result

Structure-Based Optimization of Bisphosphonate Nucleoside Inhibitors of Human 5(3)-deoxyribonucleotidases

of inhibitory compounds. In this work, bisphosphonate nucleoside derivatives were designedCellular 5-nucleotidases, enzymes regulating nucleotide/nucleoside pools, are capable of dephosphorylating phosphomonoesters of impo...

Organic chemistry

  • 2018
  • Jimp
  • Link
Result

Bifunctional acyclic nucleoside phosphonates: synthesis of chiral 9-{3-hydroxy[1,4-bis(phosphonomethoxy)]butan-2-yl} derivatives of purines

We report here a general method for the synthesis of new type of chiral acyclic nucleoside four-carbon bisphosphonates, (2S,3S) or (2R,3R)-9-{3-(hydroxy)-1,4-[bis(phosphonomethoxy]butan-2-yl} derivative of purines respectively. L-Th...

CC - Organická chemie

  • 2007
  • Jx
Result

Acyclic nucleoside bisphosphonates: Synthesis and properties of chiral 2-amino-4,6-bis[(phosphonomethoxy)alkoxy]pyrimidines

2-Amino-4,6-bis[(phosphonomethoxy)alkoxy]pyrimidines bearing two equal or different achiral or chiral phosphonoalkoxy chains have been prepared either by aromatic nucleophilic substitution of 2-amino-4,6-dichloropyrimidine or by alkylation of 4,6-dih...

CC - Organická chemie

  • 2009
  • Jx
Result

Bifunctional acyclic nucleoside phosphonates: 2. Symmetrical 2-{[bis(phosphono)methoxy]methyl}ethyl derivatives of purines and pyrimidines

Novel series of symmetrial 2-{[bis(phosphonomethoxy)methyl]ethyl} N9-substituted purines and N1-substituted pyrimidines were prepared and evaluated for the biological activity....

CC - Organická chemie

  • 2007
  • Jx
Result

Synthesis of phosphonomethoxyethyl or 1,3-bis(phosphonomethoxy)propan-2-yl lipophilic esters of acyclic nucleoside phosphonates

A new alternative synthetic pathway towards mono and diesters of acyclic nucleoside phosphonates (PMEA, PMEC and PMEG) or [1,3-bis(phosphonomethoxy)propan-2-yl]adenine bearing one or two hexadecyloxypropyl ester groups (CH2)3O-n-C16H33 is re...

CC - Organická chemie

  • 2007
  • Jx
Result

Synthesis and properties of chiral open-ring acyclic nucleoside bisphosphonates

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 cultu...

CC - Organická chemie

  • 2005
  • D
Result

Structure-based design of a bisphosphonate 5'(3')-deoxyribonucleotidase inhibitor

Cellular 5'-nucleotidases regulating nucleotide/nucleoside pools are capable of dephosphorylating phosphomonoesters of important nucleoside analogue drugs, thus decreasing their therapeutic efficacy. Based on previously known inhibi...

CE - Biochemie

  • 2015
  • Jx
  • Link
Result

Synthesis and Evaluation of Asymmetric Acyclic Nucleoside Bisphosphonates as Inhibitors of Plasmodium falciparum and Human Hypoxanthine-Guanine-(Xanthine) Phosphoribosyltransferase

Acyclic nucleoside bisphosphonates (ANbPs) have previously been shown to be good inhibitors of human hypoxanthine-guanine phosphoribosyltransferase (HGPRT) and Plasmodium falciparum (Pf) hypoxanthine-guanine-xanthine phosphoribosylt...

Organic chemistry

  • 2017
  • Jimp
  • Link
Result

Synthesis of Tetrasubstituted Thiophenes via Direct Metalation

Thiophene moiety can be derivatized by various synthetic procedures. The most convenient method seems to be derivatization via direct metalation, but synthesis of polysubstituted thiophenes bearing reactive groups is difficult because of high reactiv...

Organic chemistry

  • 2020
  • Jimp
  • Link
Result

N2'-Branched Acyclic Nucleoside Phosphonates Containing 9-Deazahypoxanthine as Inhibitors of Plasmodium falciparum 6-Oxopurine Phosphoribosyltransferase

Twelve N2'-branched acyclic nucleoside phosphonates and bisphosphonates were synthesized as potential inhibitors of Plasmodium falciparum hypoxanthine-guanine-xanthine phosphoribosyltransferase (PfHGXPRT), the key enzyme in the puri...

Organic chemistry

  • 2023
  • Jimp
  • Link
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