Student or educator? Sign up with your school email and get 6 months of Pro free.
CoChat
Sign Up
Cited by 455

The DOI matches its Crossref record.

First Non-ATP Competitive Glycogen Synthase Kinase 3 β (GSK-3β) Inhibitors: Thiadiazolidinones (TDZD) as Potential Drugs for the Treatment of Alzheimer's Disease

Open access
Martinez, Ana, Alonso, Mercedes, Castro, Ana, Pérez, Concepción, Moreno, Francisco J.·2002·Journal of Medicinal Chemistry
DOI 10.1021/jm011020u
Open this paper in CoChat — free account

Abstract

Glycogen synthase kinase 3 beta (GSK-3beta) has a central role in Alzheimer's disease (AD). Selective inhibitors which avoid tau hyperphosphorylation may represent an effective therapeutical approach to the AD pharmacotherapy and other neurodegenerative disorders. Here, we describe the synthesis, biological evaluation, and SAR of the small heterocyclic thiadiazolidinones (TDZD) as the first non-ATP competitive inhibitor of GSK-3beta. Their synthesis is based on the reactivity of sulfenyl chlorides. In GSK-3beta assays, TDZD derivatives showed IC(50) values in the micromolar range, whereas in other protein kinases assays they were devoid of any inhibitory activity. SAR studies allowed the identification of the key structural features. Finally, a possible enzymatic binding mode is proposed.

Overview

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

A few free checks a day · papers already verified open instantly · results are public

Integrity signals

Registry

Crossref · 10.1021/jm011020u

Cites

Statistics

Verification

Claims the paper makes

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

A few free checks a day · papers already verified open instantly · results are public

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

The self-check needs the paper’s full text.

Citations

Cites

No references could be resolved yet.

Research works printed but not linked: 36

  1. Brion J. P., 2001, Neurofibrillary Tangles and Tau Phosphorylation. Biochem. Soc. Symp.
  2. Alonso A., 2001, Proc. Natl. Acad. Sci. U.S.A., 98, 6928
  3. Anderton B. H., 2001, M. Sites of Phosphorylation in Tau and Factors Affecting Their Regulation. Biochem. Soc. Symp.
  4. Larner A. J, 1999, Expert Opin. Ther. Pat., 9, 1370, 10.1517/13543776.9.10.1359 · DOI
  5. Castro A., 2000, Expert Opin. Ther. Pat., 10, 1527
  6. Imahori K., 1997, J. Biochem., 121, 188
  7. Flaherty D. B., 2000, J. Neurosci. Res., 62, 472, 10.1002/1097-4547(20001101)62:3<463::AID-JNR16>3.0.CO;2-7 · DOI
  8. Spittaels K., 2000, J. Biol. Chem., 275, 41349, 10.1074/jbc.M006219200 · DOI · Paper page
  9. Anderton B. H., 2000, Mol. Med. Today, 6, 59, 10.1016/S1357-4310(99)01640-8 · DOI
  10. Takashima A., 1998, Proc. Natl. Acad. Sci. U.S.A., 95, 9641, 10.1073/pnas.95.16.9637 · DOI · Paper page
  11. Applin A. E., 1997, Neuroreport, 8, 643
  12. Ferkey D. M., 2000, Dev. Biol., 225, 479, 10.1006/dbio.2000.9816 · DOI
  13. Lau K. F., 1999, J. Pept. Res., 54, 91
  14. Lucas J. J., 2001, EMBO J., 20, 39
  15. Ter Haar E., 2001, Nat. Struct. Biol., 8, 596, 10.1038/89624 · DOI
  16. Dajani R., 2001, Cell, 105, 732, 10.1016/S0092-8674(01)00374-9 · DOI · Paper page
  17. Frame S., 2001, Mol. Cell, 7, 1327, 10.1016/S1097-2765(01)00253-2 · DOI · Paper page
  18. Harwood A. J, 2001, Cell, 105, 824, 10.1016/S0092-8674(01)00412-3 · DOI · Paper page
  19. Muñoz-Montaño J. R., 1997, FEBS Lett., 411, 188
  20. Takahashi M., 1999, J. Neurochem., 73, 2083
  21. Hers I., 1999, FEBS Lett., 460, 436, 10.1016/S0014-5793(99)01389-7 · DOI
  22. Smith D. G., 2001, Bioorg. Med. Chem. Lett., 11, 639
  23. Leost M., 2000, Eur. J. Biochem., 267, 5994, 10.1046/j.1432-1327.2000.01673.x · DOI · Paper page
  24. Leclercq S., 2001, J. Biol. Chem., 276, 260
  25. Meijer L., 2000, Chem. Biol., 7, 63, 10.1016/S1074-5521(00)00063-6 · DOI · Paper page
  26. Martinez A., 2000, May
  27. Ottman G., 1966, N-Aryl and N-Alkyl-S-Chloroisothiocarbamoyl Chlorides with Isocyantes. Synthesis of 1,2,4-Thiadiazolidine-3,5-diones. Angew. Chem., Int. Ed. Engl., 5, 673
  28. Martinez A., 1997, Bioorg. Med. Chem., 5, 1283, 10.1016/S0968-0896(97)00077-1 · doi:10.1016/s0968-0896(97)00077-1
  29. Martinez A., 1999, Arch. Pharm. Pharm. Med. Chem., 332, 194
  30. Martinez A., 2000, Eur. J. Med. Chem., 35, 922, 10.1016/S0223-5234(00)01166-1 · DOI
  31. Kaugars G., 1992, J. Org. Chem., 57, 1676, 10.1021/jo00032a014 · doi:10.1021/jo00032a014
  32. Woodgett J. R, 1989, Anal. Biochem., 180, 241, 10.1016/0003-2697(89)90423-5 · DOI
  33. Garcia-Echevarria C., 2000, Med. Res. Rev., 20, 57
  34. Belmont L. D., 1996, Cell, 84, 631, 10.1016/S0092-8674(00)81037-5 · DOI · Paper page
  35. Walsh M. P., 1984, Biochem. J., 224, 127, 10.1042/bj2240117 · DOI · Paper page
  36. Alcazar A., 1988, Neurochem. Res., 13, 836, 10.1007/BF00970750 · doi:10.1007/bf00970750

Cited by

See all 455

Metadata

Authors
Martinez, A., Alonso, M., Castro, A., Pérez, C., & Moreno, F. J.
Venue
Journal of Medicinal Chemistry
Publisher
American Chemical Society (ACS)
Published
2002-02-13
Volume
45
Issue
6
Pages
1292-1299
ISSN
  • 0022-2623 (ISSN-L)
  • 1520-4804
DOI
10.1021/jm011020u
OpenAlex
W1995377960
Cited by
455
References
0
FWCI
10.29
Type
journal article
Language
en
Open access
green

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review

How to cite

Cite CoChat for the checks on this page, and the paper for its own findings.

This page
CoChat. (2026). Citation check: First Non-ATP Competitive Glycogen Synthase Kinase 3 β (GSK-3β) Inhibitors: Thiadiazolidinones (TDZD) as Potential Drugs for the Treatment of Alzheimer's Disease. https://app.cochat.ai/papers/10.1021/jm011020u
The paper
Martinez, A., Alonso, M., Castro, A., Pérez, C., & Moreno, F. J. (2002). First Non-ATP Competitive Glycogen Synthase Kinase 3 β (GSK-3β) Inhibitors: Thiadiazolidinones (TDZD) as Potential Drugs for the Treatment of Alzheimer's Disease. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm011020u

Data sources

Bibliographic data: Semantic Scholar, OpenAlex, Crossref.

Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.