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

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Pharmaceutical Chemistry Journal Aims and scope

We report here studies of the antitumor action of a 4H-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 4H-aminochromene compound AKh-554 to be regarded as having potential for development of molecularly targeted drugs.

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Authors and Affiliations

  1. All-Union Science Center for the Safety of Biologically Active Substances, 23 Kirov Street, Staraya Kupavna, 1452850, Moscow Oblast, Russia

    E. A. Samyshina, S. Ya. Skachilova, E. A. Simakina & E. V. Shilova

  2. I. M. Sechenov First Moscow State Medical University, Russian Ministry of Health (Sechenov University), 8/2 Trubetskaya Street, 119991, Moscow, Russia

    E. V. Blinova, M. Yu. Kudryavtsev, D. N. Shimanovskii, A. A. Epishkina & K. K. Arutyunyan

  3. Dmitrii Rogachev National Medical Research Center for Pediatric Oncology, Hematology, and Immunology, Russian Ministry of Health, 1 Samora Machel Street, 117997, Moscow, Russia

    D. S. Blinov, Yu. A. Shifrin & A. A. Makhrova

  4. N. P. Ogarev National Mordovan State Research University, 68 Bol’shevistskaya Street, 430005, Saransk, Russia

    O. M. Tumutolova & O. N. Deryabina

Authors
  1. E. A. Samyshina
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  2. E. V. Blinova
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  3. M. Yu. Kudryavtsev
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  4. D. N. Shimanovskii
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  5. S. Ya. Skachilova
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  6. A. A. Epishkina
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  7. D. S. Blinov
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  8. O. M. Tumutolova
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  9. E. A. Simakina
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  10. Yu. A. Shifrin
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  11. O. N. Deryabina
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  12. E. V. Shilova
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  13. A. A. Makhrova
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  14. K. K. Arutyunyan
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Corresponding author

Correspondence to D. S. Blinov.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 56, No. 1, pp. 15 – 18, January, 2022.

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Samyshina, E.A., Blinova, E.V., Kudryavtsev, M.Y. et al. Preparation and Mechanism of the Antitumor Action of a 4H-Aminochromene Compound. Pharm Chem J 56, 12–15 (2022). https://doi.org/10.1007/s11094-022-02593-3

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  • DOI: https://doi.org/10.1007/s11094-022-02593-3

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