Biopolym. Cell. 2022; 38(1):37-47.
Bioorganic Chemistry
The effect of heterocyclic substituent at C-3 position of 1-(4-methyl-piperazin-1-yl)isoquinolines on their anticancer activity
1Konovalenko A. S., 1Zhirnov V. V., 1Shablykin O. V., 1, 2Shablykina O. V., 1, 2Moskvina V. S., 1Brovarets V. S.
  1. V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine,
    1, Murmans'ka Str., Kyiv, Ukraine, 02094
  2. Taras Shevchenko National University of Kyiv
    64, Volodymyrska Str., Kyiv, Ukraine, 01601


Aim. A comparative analysis of the anti-cancer activity of 1-(4-methylpiperazin-1-yl)isoquinolines with different heteroaromatic substituents in C-3 position: 2-methylthiazol-4-yl, 2-phenylthiazol-4-yl, 2-(pyridin-4-yl)thiazol-4-yl, imi-dazo[2,1-b]thiazol-6-yl, quinoxalin-2-yl, 6,7-dimethylquinoxalin-2-yl. Methods. Biological tests; statistic methods. Results. In vitro screening of the anticancer activity showed that the derivatives with 2-phenylthiazol-4-yl, quinoxaline-2-yl, 6,7-dimethylquinoxalin-2-yl substituents demonstrated the highest level of anticancer activity; however, they were inferior to 2-(pyridin-4-yl)thiazol-4-yl. The product with the 2-methylthiazol-4-yl residue almost did not demonstrated cytotoxicity. Comparative analysis showed no significant correlation with known drugs; hence these compounds have specific molecular targets. Conclusions. The resulting 1-amino-3-hetarylisoquinolines are a promising class of compounds for anticancer drug development. The level and direction of the activity significantly depend on the nature of heterocyclic substituents.
Keywords: in vitro screening, anticancer activity, 1-amino-3-hetarylisoquinolines