Design, synthesis and biological evaluation of 2,3-dihydroimidazo[2,1-b]thiazoles as dual EGFR and IGF1R inhibitors.

doi:10.1016/j.bioorg.2021.105151

Paper

Design, synthesis and biological evaluation of 2,3-dihydroimidazo[2,1-b]thiazoles as dual EGFR and IGF1R inhibitors.

Published Jul 7, 2021 · Pradip K Gadekar, Ganesh Urunkar, Abhijit Roychowdhury

Bioorganic chemistry

Q1 SJR score

14

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1

Influential Citations

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Abstract

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In Vitro Study

Study Snapshot

The 2,3-dihydroimidazo[2,1-b]thiazoles show promising activity as dual EGFR and IGF1R inhibitors, with promising activity against both wild-type and T790M mutant forms of enzymes.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Design, synthesis and biological evaluation of 2,3-dihydroimidazo[2,1-b]thiazoles as dual EGFR and IGF1R inhibitors.

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References

Citations

Pyrimidine-based dual-target inhibitors targeting epidermal growth factor receptor for overcoming drug resistance in cancer therapy(2006-present).

Pyrimidine-based dual-target inhibitors targeting epidermal growth factor receptor offer a promising cancer treatment option with reduced resistance, lower dosage requirements, and reduced toxicity profiles.

Recent studies on protein kinase signaling inhibitors based on thiazoles: review to date

Thiazole-based compounds show potential as anti-cancer agents by targeting various protein kinases, including serine/threonine and tyrosine kinases.

Synthesis, molecular modeling simulations and anticancer activity of some new Imidazo[2,1-b]thiazole analogues as EGFR/HER2 and DHFR inhibitors.

New imidazo[2,1-b]thiazole analogues show promising anticancer activity, with compounds 23 and 39 showing potent activity against MCF-7 breast cancer cells and showing in vivo anticancer activity in mice.

Epidermal growth factor receptor dual-target inhibitors as a novel therapy for cancer: A review.

EGFR dual-target inhibitors show promise as a more effective and less resistant cancer therapy, offering new options for patients with previously untreatable malignancies.

Design, synthesis and biological evaluation of novel spiro-quinazolinone derivatives as chitin synthase inhibitors and antifungal agents.

Novel spiro-quinazolinone derivatives show selective and broad-spectrum antifungal activity, potentially acting as lead compounds against drug-resistant fungi.

New thiazole-based derivatives as EGFR/HER2 and DHFR inhibitors: Synthesis, molecular modeling simulations and anticancer activity.

New thiazole-based derivatives show promising anticancer activity, particularly MCF-7 breast cancer, with high safety and selectivity indices.

An Overview of the Biological Evaluation of Selected Nitrogen-Containing Heterocycle Medicinal Chemistry Compounds

Recent studies in biological assessment of nitrogen-containing heterocycle compounds show promising potential for drug discovery and smart biomimetics.