New Dimethylpyridine-3-Carboxamide Derivatives as MMP-13 Inhibitors with Anticancer Activity

A series of dimethylpyridine-3-carboxamide derivatives was designed as potential, selective, non-zinc chelating inhibitors of matrix metalloproteinase 13 (MMP-13), and subsequently synthesized. The identity of the obtained compounds was confirmed by FT-IR, <sup>1</sup>H/<sup>13</sup>C NMR, and HR-MS methods. Fluorescence spectroscopy was applied to study the interaction of synthesized compounds with human serum albumin, providing insight into their potential transport properties in plasma. In parallel, the electronic properties and reactivity parameters relevant to enzyme binding of the designed molecules were analyzed using density functional theory. Molecular docking and molecular dynamics simulations revealed the compounds to interact preferentially and stably within the S<sub>1</sub> pocket of MMP-13 via hydrogen bonds and π-stacking interactions. The calculated binding free energy confirmed the stability and persistence of the complexes during simulation, indicating a strong and specific recognition pattern. On the other hand, their affinity towards MMP-8 was considerably weaker, which is consistent with the predicted selectivity profile. In addition, the biological evaluation confirmed MMP-13 inhibition. Finally, in vitro tests revealed their cytotoxic activity against cancer cell lines.

Authors

Institutions

Publication Details

Journal
Molecules
Published
2025-12-05
DOI
https://doi.org/10.3390/molecules30244662
Primary Topic
Protease and Inhibitor Mechanisms
Type
article
Field-Weighted Citation Impact
0.00
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

New Dimethylpyridine-3-Carboxamide Derivatives as MMP-13 Inhibitors with Anticancer Activity

Żaneta Czyżnikowska, Piotr Świątek, Aleksandra Kotynia, Remigiusz Płaczek et al.
Molecules
Protease and Inhibitor Mechanisms
article

New Dimethylpyridine-3-Carboxamide Derivatives as MMP-13 Inhibitors with Anticancer Activity

Żaneta Czyżnikowska, Piotr Świątek, Aleksandra Kotynia, Remigiusz Płaczek, Tomasz Janek, Małgorzata Strzelecka
article en

Abstract

A series of dimethylpyridine-3-carboxamide derivatives was designed as potential, selective, non-zinc chelating inhibitors of matrix metalloproteinase 13 (MMP-13), and subsequently synthesized. The identity of the obtained compounds was confirmed by FT-IR, <sup>1</sup>H/<sup>13</sup>C NMR, and HR-MS methods. Fluorescence spectroscopy was applied to study the interaction of synthesized compounds with human serum albumin, providing insight into their potential transport properties in plasma. In parallel, the electronic properties and reactivity parameters relevant to enzyme binding of the designed molecules were analyzed using density functional theory. Molecular docking and molecular dynamics simulations revealed the compounds to interact preferentially and stably within the S<sub>1</sub> pocket of MMP-13 via hydrogen bonds and π-stacking interactions. The calculated binding free energy confirmed the stability and persistence of the complexes during simulation, indicating a strong and specific recognition pattern. On the other hand, their affinity towards MMP-8 was considerably weaker, which is consistent with the predicted selectivity profile. In addition, the biological evaluation confirmed MMP-13 inhibition. Finally, in vitro tests revealed their cytotoxic activity against cancer cell lines.

MoleculesVol. 30(24)
Wrocław University of Environmental and Life Sciences (PL), Wroclaw Medical University (PL)
Openalex Percentile: Top 53%
Protease and Inhibitor Mechanisms
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.

New Dimethylpyridine-3-Carboxamide Derivatives as MMP-13 Inhibitors with Anticancer Activity — Żaneta Czyżnikowska, Piotr Świątek, et al. · Molecules (2025) | TGRS Research Map | TGRS