Preparation and Mechanism of the Antitumor Action of a 4H-Aminochromene Compound

We report here studies of the antitumor action of a 4 H -aminochromene compound in a xenograft model of ALK-expressing lung adenocarcinoma in humanized nude BALB/c mice. These studies showed that intragastric administration of the compound produced dose-dependent reductions in tumor size and metasta...

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Published inPharmaceutical chemistry journal Vol. 56; no. 1; pp. 12 - 15
Main Authors Samyshina, E. A., Blinova, E. V., Kudryavtsev, M. Yu, Shimanovskii, D. N., Skachilova, S. Ya, Epishkina, A. A., Blinov, D. S., Tumutolova, O. M., Simakina, E. A., Shifrin, Yu. A., Deryabina, O. N., Shilova, E. V., Makhrova, A. A., Arutyunyan, K. K.
Format Journal Article
LanguageEnglish
Published New York Springer US 01.04.2022
Springer
Subjects
Cell death
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
synthesis
4
xenograft
antitumor action
aminochromene compound
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Summary:We report here studies of the antitumor action of a 4 H -aminochromene compound in a xenograft model of ALK-expressing lung adenocarcinoma in humanized nude BALB/c mice. These studies showed that intragastric administration of the compound produced dose-dependent reductions in tumor size and metastasis frequency, with increases in the survival of xenograft-carrying animals. The effect of the compound is based on suppression of the expression of receptor tyrosine kinase and β3-tubulin in tumor tissues and activation of caspase-3-dependent programmed tumor cell death. The results allow the 4 H -aminochromene compound AKh-554 to be regarded as having potential for development of molecularly targeted drugs.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-022-02593-3