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Inhibition of Cdk Activity

Inhibition of Cdk Activity

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Related Experiment Video

Updated: Jun 5, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Published on: February 9, 2021

Third-Generation CD73 Inhibitors Based on a 4,6-Disubstituted-2-Thiopyridine Scaffold.

Félix Grosjean¹, Maria Shaldaeva², Emeline Cros-Perrial³

¹Institut des Biomolécules Max Mousseron (IBMM), Pôle Chimie Balard, Univ. Montpellier, CNRS, ENSCM, 34293, Montpellier, France.

|December 13, 2024

Summary

New thiopyridine derivatives were synthesized and tested as ecto-5'-nucleotidase (CD73) inhibitors. Some compounds effectively antagonized T-cell proliferation inhibition, showing potential therapeutic applications.

Keywords:

5’-ectonucleotidase Adenosine receptors Enzyme inhibitor Medicinal chemistry Nitrogen heterocycles Thiopyridine

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Published on: June 20, 2014

Area of Science:

Medicinal Chemistry
Immunology
Biochemistry

Background:

Ecto-5'-nucleotidase (CD73) is a key enzyme in purinergic signaling, often targeted in immune modulation.
T-cell proliferation is crucial for immune responses and can be modulated by CD73 activity.
Developing novel CD73 inhibitors is of interest for therapeutic interventions.

Purpose of the Study:

To synthesize and evaluate novel 4,6-disubstituted-2-thiopyridine derivatives as potential CD73 inhibitors.
To investigate the structure-activity relationships of these derivatives.
To assess their impact on T-cell proliferation and potential off-target effects.

Main Methods:

Synthesis of approximately ninety 4,6-disubstituted-2-thiopyridine derivatives.
Functional assay on immune cells to measure T-cell proliferation inhibition.
Inhibition assays on human adenosine A2A receptor (hA2A) in HEK-293 cells.

Main Results:

Several thiopyridine derivatives were synthesized using efficient one- or two-step procedures.
Compounds 4 9ab and 4 9ai demonstrated significant antagonism of T-cell proliferation inhibition at 100 μM and 10 μM concentrations.
These active compounds also exhibited moderate inhibition of the hA2A receptor in the micromolar range.

Conclusions:

The synthesized 4,6-disubstituted-2-thiopyridine derivatives show promise as CD73 inhibitors.
Compounds 4 9ab and 4 9ai possess dual activity, inhibiting CD73 and moderately affecting the hA2A receptor.
Further optimization could lead to more selective and potent inhibitors with reduced molecular size and lipophilicity.