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Design, synthesize, and evaluate novel imidazo[4,5-b]pyridine-acrylonitrile derivatives as VEGFR-2 inhibitors targeting breast and liver cancer cell lines.

September 17, 2026Drug Development Research

Design, Synthesis, In Vitro Biological Evaluation, and In Silico Studies of Novel Imidazo4,5‐ b Pyridine‐Acrylonitrile‐Based Derivatives as VEGFR‐2 Inhibitors Against Breast Cancer and Hepatocellular Carcinoma

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Authors

LMLamia W. Mohamed ASAhmed A. Saadeldin AFAyman Farag

Discussion

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Overview

In vitro study demonstrates potent VEGFR-2 inhibition and cytotoxicity in breast and liver cancer cells, indicating therapeutic potential against tumor angiogenesis.

Key Points

Design, synthesize, and evaluate novel imidazo[4,5-b]pyridine-acrylonitrile derivatives as VEGFR-2 inhibitors targeting breast and liver cancer cell lines.
Synthesized 22 imidazo[4,5-b]pyridine-acrylonitrile-based derivatives and screened their enzyme inhibitory activity against VEGFR-2.
Assessed in vitro cytotoxic activity of four lead derivatives against MCF-7 breast cancer and HepG2 hepatocellular carcinoma cell lines in comparison with sorafenib.
Conducted cell cycle analysis, apoptosis assays, and in silico docking and pharmacokinetic predictions for the top candidate, compound 2f.
Seven derivatives exhibited potent VEGFR-2 inhibition with IC50 values between 0.029 and 0.087 µM, surpassing the reference drug sorafenib (IC50 = 0.091 µM).
Lead compound 2f showed potent VEGFR-2 inhibition (IC50 = 0.029 µM) and cytotoxicity against MCF-7 (IC50 = 0.073 µM) and HepG2 (IC50 = 0.09 µM) compared to sorafenib (IC50 = 0.16 µM and 0.19 µM, respectively).
Compound 2f induced 13.67% cell cycle arrest at the G2/M phase, stimulated apoptosis, and demonstrated favorable active-site binding scores alongside predicted oral bioavailability.

Cite This Study

Mohamed et al. (2026) studied this question.

synapsesocial.com/papers/6aabb7f75f706d05830e74e4 https://doi.org/10.1002/ddr.70385

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September 17, 2026Drug Development Research

Design, Synthesis, In Vitro Biological Evaluation, and In Silico Studies of Novel Imidazo4,5‐ b Pyridine‐Acrylonitrile‐Based Derivatives as VEGFR‐2 Inhibitors Against Breast Cancer and Hepatocellular Carcinoma

View Full Paper

Ask AI

Bookmark

Authors

LMLamia W. Mohamed ASAhmed A. Saadeldin AFAyman Farag

Discussion

Member takes

Overview

In vitro study demonstrates potent VEGFR-2 inhibition and cytotoxicity in breast and liver cancer cells, indicating therapeutic potential against tumor angiogenesis.

Key Points

Design, synthesize, and evaluate novel imidazo[4,5-b]pyridine-acrylonitrile derivatives as VEGFR-2 inhibitors targeting breast and liver cancer cell lines.
Synthesized 22 imidazo[4,5-b]pyridine-acrylonitrile-based derivatives and screened their enzyme inhibitory activity against VEGFR-2.
Assessed in vitro cytotoxic activity of four lead derivatives against MCF-7 breast cancer and HepG2 hepatocellular carcinoma cell lines in comparison with sorafenib.
Conducted cell cycle analysis, apoptosis assays, and in silico docking and pharmacokinetic predictions for the top candidate, compound 2f.
Seven derivatives exhibited potent VEGFR-2 inhibition with IC50 values between 0.029 and 0.087 µM, surpassing the reference drug sorafenib (IC50 = 0.091 µM).
Lead compound 2f showed potent VEGFR-2 inhibition (IC50 = 0.029 µM) and cytotoxicity against MCF-7 (IC50 = 0.073 µM) and HepG2 (IC50 = 0.09 µM) compared to sorafenib (IC50 = 0.16 µM and 0.19 µM, respectively).
Compound 2f induced 13.67% cell cycle arrest at the G2/M phase, stimulated apoptosis, and demonstrated favorable active-site binding scores alongside predicted oral bioavailability.

Cite This Study

Mohamed et al. (2026) studied this question.

synapsesocial.com/papers/6aabb7f75f706d05830e74e4 https://doi.org/10.1002/ddr.70385

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