Anticancer activity studies of isoquinoline derivatives – products of 3 (2-(thien-2-yl)thiazol-4-yl)isocoumarin recyclization
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A synthetic methodology for obtaining 1-functionalized isoquinolines starting with
3-hetarylisocoumarin has been developed. Studies of anticancer activity of 3-(2-(thien-2-yl)thiazol-4-yl)isocoumarin and the obtained derivatives have been performed on 60 lines of cancer cells in Cancer National Institute of the USA. The obtained compounds demonstrated a clear and strong correlation between anticancer activity and the character of substituents in the base structure, possessed a very low cytotoxicity, and performed well against several cancer types.
[1] My Van, H. T., Woo, H., Jeong, H. M., Khadka, D. B., Yang, S. H., Zhao, C., Jin, Y., Lee, E.-S., Lee, K. Y., Kwon, Y., Cho, W.-J. (2014). Design, synthesis and systematic evaluation of cytotoxic 3-heteroarylisoquinolinamines as topoisomerases inhibitors. Eur. J. Med. Chem., Vol. 82, pp. 181–194. doi: https://doi.org/10.1016/j.ejmech.2014.05.047.
[2] Shablykina, O. V., Shablykin, O. V., Ishchenko, V. V. Voronaya, A. V., Khilya, V. P. (2013). Synthesis of 3-hetaryl-1H-isochromen-1-ones based on 3-(2-bromoacetyl)-1H-isochromen-1-one. Chem. Heterocycl. Compd., Vol. 48, Iss. 11, pp. 1621–1627. doi: https://doi.org/10.1007/s10593-013-1183-7.
[4] https://dtp.cancer.gov/discovery_development/nci-60/default.html
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