Page last updated: 2024-09-03

wr 99210 and cycloguanil

wr 99210 has been researched along with cycloguanil in 22 studies

Compound Research Comparison

Studies
(wr 99210)
Trials
(wr 99210)
Recent Studies (post-2010)
(wr 99210)
Studies
(cycloguanil)
Trials
(cycloguanil)
Recent Studies (post-2010) (cycloguanil)
590122311637

Protein Interaction Comparison

ProteinTaxonomywr 99210 (IC50)cycloguanil (IC50)
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)5.8
Bifunctional dihydrofolate reductase-thymidylate synthasePlasmodium falciparum K12.985
Dihydrofolate reductasePneumocystis carinii0.45
Dihydrofolate reductaseRattus norvegicus (Norway rat)0.11

Research

Studies (22)

TimeframeStudies, this research(%)All Research%
pre-19902 (9.09)18.7374
1990's4 (18.18)18.2507
2000's12 (54.55)29.6817
2010's3 (13.64)24.3611
2020's1 (4.55)2.80

Authors

AuthorsStudies
Genther, CS; Smith, CS1
Ager, AL; Bliss, RA; Canfield, CJ; Jacobus, DP; Jensen, NP; Kotecka, BM; Rieckmann, KH; Terpinski, J1
Chitnumsub, P; Kamchonwongpaisan, S; Sirawaraporn, W; Taylor, P; Vanichtanankul, J; Walkinshaw, MD; Yuthavong, Y; Yuvaniyama, J1
Ferrari, AM; Pacchioni, S; Parenti, MD; Rastelli, G1
Diaz, DS; Jacobus, DP; Kozar, MP; Milhous, WK; O'Neil, MT; Schiehser, GA; Shearer, TW; Skillman, DR; Smith, PL; Yang, YS1
Brun, R; Chitnumsub, P; Dartois, V; Diagana, TT; Goh, A; Kamchonwongpaisan, S; Keller, TH; Kiara, SM; Lakshminarayana, SB; Ma, NL; Maneeruttanarungroj, C; Nzila, A; Rottmann, M; Taweechai, S; Weaver, M; Wittlin, S; Wong, J; Yeung, BK; Yuthavong, Y; Zou, B1
Adams, JH; Auliff, AM; Cheng, Q; O'Neil, MT1
Arwon, U; Charoensetakul, N; Kamchonwongpaisan, S; Rattanajak, R; Srisuwannaket, C; Tarnchompoo, B; Taweechai, S; Thongpanchang, C; Vanichtanankul, J; Vilaivan, T; Vitsupakorn, D; Yuthavong, Y1
Howells, RE; Judge, BM1
Ager, AL; Canfield, CJ; Jacobus, DP; Lewis, NJ; Milhous, WK; Rossan, RN; Sweeney, TR1
Christopherson, RI; Yeo, AE1
Fidock, DA; Nomura, T; Wellems, TE1
Howard, V; Mookherjee, S; Nzila-Mouanda, A; Sibley, CH; Watkins, W1
Kamchonwongpaisan, S; Lowe, G; Quarrell, R; Rastelli, G; Sirawaraporn, W; Sompornpisut, P; Thebtaranonth, Y; Vilaivan, T; Yuthavong, Y1
Hankins, EG; Sibley, CH; Warhurst, DC1
Delfino, RT; Figueroa-Villar, JD; Santos-Filho, OA1
Hastings, MD; Sibley, CH1
Hunt, SY; Rezvani, BB; Sibley, CH1
Anh, le N; Auliff, A; Bell, D; Chen, N; Cheng, Q; Gao, Q; Maguire, J; O'Neil, MT; Russell, B; Wilson, DW1
Chitnumsub, P; Kamchonwongpaisan, S; Taweechai, S; Vanichtanankul, J; Yuthavong, Y1
Asher, CO; Diaz, DS; Jacobus, DP; Kozar, MP; Milhous, WK; Schiehser, GA; Shearer, TW; Skillman, DR; Smith, KS; Sousa, JC1
Adams, JH; Auliff, AM; Balu, B; Chen, N; Cheng, Q; O'Neil, MT1

Other Studies

22 other study(ies) available for wr 99210 and cycloguanil

ArticleYear
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
    Journal of medicinal chemistry, 1977, Volume: 20, Issue:2

    Topics: Animals; Antimalarials; Bacteria; Drug Resistance, Microbial; Escherichia coli; Folic Acid; Folic Acid Antagonists; Malaria; Mice; Plasmodium berghei; Triazines

1977
Phenoxypropoxybiguanides, prodrugs of DHFR-inhibiting diaminotriazine antimalarials.
    Journal of medicinal chemistry, 2001, Nov-08, Volume: 44, Issue:23

    Topics: Animals; Antimalarials; Drug Evaluation, Preclinical; Female; Folic Acid Antagonists; Guanidines; Malaria; Male; Mice; Plasmodium berghei; Plasmodium falciparum; Prodrugs; Proguanil; Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Triazines

2001
Insights into antifolate resistance from malarial DHFR-TS structures.
    Nature structural biology, 2003, Volume: 10, Issue:5

    Topics: Amino Acid Sequence; Animals; Conserved Sequence; Drug Resistance; Folic Acid Antagonists; Models, Molecular; Molecular Sequence Data; Multienzyme Complexes; Plasmodium; Plasmodium falciparum; Protein Conformation; Sequence Alignment; Sequence Homology, Amino Acid; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase

2003
Three-dimensional quantitative structure-activity relationship analysis of a set of Plasmodium falciparum dihydrofolate reductase inhibitors using a pharmacophore generation approach.
    Journal of medicinal chemistry, 2004, Aug-12, Volume: 47, Issue:17

    Topics: Aldehyde Reductase; Animals; Antimalarials; Binding Sites; Folic Acid Antagonists; Models, Molecular; Plasmodium falciparum; Quantitative Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase

2004
In vitro metabolism of phenoxypropoxybiguanide analogues in human liver microsomes to potent antimalarial dihydrotriazines.
    Journal of medicinal chemistry, 2005, Apr-21, Volume: 48, Issue:8

    Topics: Animals; Antimalarials; Biguanides; Chromatography, Liquid; Drug Resistance; Folic Acid Antagonists; Humans; In Vitro Techniques; Mass Spectrometry; Microsomes, Liver; Plasmodium falciparum; Prodrugs; Structure-Activity Relationship; Triazines

2005
Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
    Antimicrobial agents and chemotherapy, 2010, Volume: 54, Issue:6

    Topics: Administration, Oral; Animals; Antimalarials; Biological Availability; Drug Resistance; Female; Folic Acid Antagonists; Humans; In Vitro Techniques; Malaria; Malaria, Falciparum; Male; Mice; Models, Molecular; Mutation; Parasitic Sensitivity Tests; Plasmodium berghei; Plasmodium falciparum; Pyrimethamine; Quinazolines; Rats; Rats, Wistar; Tetrahydrofolate Dehydrogenase

2010
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
    Antimicrobial agents and chemotherapy, 2010, Volume: 54, Issue:9

    Topics: Animals; Folic Acid Antagonists; Multienzyme Complexes; Mutation; Parasitic Sensitivity Tests; Plasmodium falciparum; Plasmodium vivax; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Transfection

2010
Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
    European journal of medicinal chemistry, 2020, Jun-01, Volume: 195

    Topics: Antimalarials; Folic Acid Antagonists; Molecular Docking Simulation; Mutation; Protein Binding; Protein Conformation; Protozoan Proteins; Tetrahydrofolate Dehydrogenase; Triazines

2020
Sustained-release implants in the chemotherapy of experimental rodent malaria I. A comparison of the effects of some antimalarials in polydimethylsiloxane matrices.
    Annals of tropical medicine and parasitology, 1981, Volume: 75, Issue:5

    Topics: Animals; Antimalarials; Chloroquine; Dimethylpolysiloxanes; Drug Implants; Malaria; Male; Mefloquine; Mice; Mice, Inbred Strains; Naphthoquinones; Piperidines; Plasmodium berghei; Primaquine; Proguanil; Pyrimethamine; Quinolines; Silicone Elastomers; Sulfadiazine; Triazines

1981
PS-15: a potent, orally active antimalarial from a new class of folic acid antagonists.
    The American journal of tropical medicine and hygiene, 1993, Volume: 49, Issue:1

    Topics: Administration, Oral; Animals; Antimalarials; Aotus trivirgatus; Atovaquone; Drug Synergism; Folic Acid Antagonists; Imides; Injections, Subcutaneous; Malaria, Falciparum; Mice; Naphthoquinones; Phenyl Ethers; Plasmodium falciparum; Proguanil; Sulfamethoxazole; Triazines

1993
Comparative effects of cycloguanil and WR99210 in human leukaemia cells and intra-erythrocytic Plasmodium.
    Annals of tropical medicine and parasitology, 1998, Volume: 92, Issue:3

    Topics: Animals; Antimalarials; Erythrocytes; Humans; Leukemia; Nucleotides; Plasmodium falciparum; Prodrugs; Proguanil; Triazines; Tumor Cells, Cultured

1998
Cycloguanil and its parent compound proguanil demonstrate distinct activities against Plasmodium falciparum malaria parasites transformed with human dihydrofolate reductase.
    Molecular pharmacology, 1998, Volume: 54, Issue:6

    Topics: Animals; Antimalarials; Folic Acid Antagonists; Genetic Complementation Test; Humans; Hypoxanthine; Inhibitory Concentration 50; Methotrexate; Mutation; Plasmodium falciparum; Proguanil; Tetrahydrofolate Dehydrogenase; Triazines

1998
Identification and analysis of dihydrofolate reductase alleles from Plasmodium falciparum present at low frequency in polyclonal patient samples.
    The American journal of tropical medicine and hygiene, 1999, Volume: 61, Issue:1

    Topics: Alleles; Animals; Antimalarials; DNA Primers; DNA Restriction Enzymes; DNA, Protozoan; Humans; Inhibitory Concentration 50; Kenya; Malaria, Falciparum; Plasmodium falciparum; Polymerase Chain Reaction; Proguanil; Pyrimethamine; Saccharomyces cerevisiae; Tetrahydrofolate Dehydrogenase; Triazines

1999
Interaction of pyrimethamine, cycloguanil, WR99210 and their analogues with Plasmodium falciparum dihydrofolate reductase: structural basis of antifolate resistance.
    Bioorganic & medicinal chemistry, 2000, Volume: 8, Issue:5

    Topics: Amino Acid Sequence; Drug Resistance; Folic Acid Antagonists; Models, Molecular; Molecular Sequence Data; Molecular Structure; Proguanil; Pyrimethamine; Sequence Homology, Amino Acid; Tetrahydrofolate Dehydrogenase; Triazines

2000
Novel alleles of the Plasmodium falciparum dhfr highly resistant to pyrimethamine and chlorcycloguanil, but not WR99210.
    Molecular and biochemical parasitology, 2001, Sep-28, Volume: 117, Issue:1

    Topics: Alleles; Amino Acid Substitution; Animals; Antimalarials; Drug Resistance; Genes, Protozoan; Inhibitory Concentration 50; Models, Molecular; Molecular Sequence Data; Parasitic Sensitivity Tests; Plasmodium falciparum; Proguanil; Protein Conformation; Pyrimethamine; Saccharomyces cerevisiae; Sequence Analysis, DNA; Tetrahydrofolate Dehydrogenase; Triazines

2001
Molecular modeling of wild-type and antifolate resistant mutant Plasmodium falciparum DHFR.
    Biophysical chemistry, 2002, Aug-02, Volume: 98, Issue:3

    Topics: Animals; Chickens; Drug Resistance; Folic Acid Antagonists; Humans; Liver; Malaria, Falciparum; Models, Chemical; Models, Genetic; Models, Molecular; Molecular Sequence Data; Plasmodium falciparum; Point Mutation; Proguanil; Pyrimethamine; Sequence Alignment; Tetrahydrofolate Dehydrogenase; Triazines

2002
Pyrimethamine and WR99210 exert opposing selection on dihydrofolate reductase from Plasmodium vivax.
    Proceedings of the National Academy of Sciences of the United States of America, 2002, Oct-01, Volume: 99, Issue:20

    Topics: Alleles; Amino Acid Sequence; Animals; Antimalarials; Dose-Response Relationship, Drug; Drug Resistance; Inhibitory Concentration 50; Malaria; Molecular Sequence Data; Mutagenesis, Site-Directed; Mutation; Plasmids; Plasmodium vivax; Point Mutation; Proguanil; Pyrimethamine; Recombinant Proteins; Sequence Homology, Amino Acid; Tetrahydrofolate Dehydrogenase; Triazines

2002
Novel alleles of Plasmodium falciparum dhfr that confer resistance to chlorcycloguanil.
    Molecular and biochemical parasitology, 2005, Volume: 139, Issue:1

    Topics: Alleles; Animals; Antimalarials; Drug Resistance; Folic Acid Antagonists; Genes, Protozoan; Mutagenesis, Site-Directed; Parasitic Sensitivity Tests; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines

2005
Amino acid mutations in Plasmodium vivax DHFR and DHPS from several geographical regions and susceptibility to antifolate drugs.
    The American journal of tropical medicine and hygiene, 2006, Volume: 75, Issue:4

    Topics: Amino Acid Sequence; Animals; Antimalarials; Asia, Southeastern; China; Dihydropteroate Synthase; Drug Combinations; Drug Resistance; Folic Acid Antagonists; Humans; Melanesia; Molecular Sequence Data; Plasmodium vivax; Point Mutation; Proguanil; Pyrimethamine; Sulfadoxine; Tetrahydrofolate Dehydrogenase; Triazines

2006
The role of tryptophan-48 in catalysis and binding of inhibitors of Plasmodium falciparum dihydrofolate reductase.
    International journal for parasitology, 2007, Volume: 37, Issue:7

    Topics: Animals; Catalysis; DNA, Protozoan; Enzyme Stability; Escherichia coli; Folic Acid Antagonists; Genetic Complementation Test; Kinetics; Mutagenesis, Insertional; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines; Tryptophan

2007
Role of specific cytochrome P450 isoforms in the conversion of phenoxypropoxybiguanide analogs in human liver microsomes to potent antimalarial dihydrotriazines.
    Drug metabolism and disposition: the biological fate of chemicals, 2008, Volume: 36, Issue:2

    Topics: Antibodies, Monoclonal; Antimalarials; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Humans; Microsomes, Liver; Prodrugs; Proguanil; Protein Isoforms; Recombinant Proteins; Triazines

2008
Functional analysis of Plasmodium vivax dihydrofolate reductase-thymidylate synthase genes through stable transformation of Plasmodium falciparum.
    PloS one, 2012, Volume: 7, Issue:7

    Topics: Amino Acid Substitution; Antimalarials; Cells, Cultured; Drug Resistance; Erythrocytes; Folic Acid Antagonists; Gene Dosage; Humans; Inhibitory Concentration 50; Mutagenesis, Insertional; Plasmodium falciparum; Plasmodium vivax; Proguanil; Protozoan Proteins; Pyrimethamine; Recombinant Proteins; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Transfection; Triazines

2012