Biopolym. Cell. 2020; 36(1):60-73.
Bioorganic Chemistry
2-(Dichloromethyl)pyrazolo[1,5-a][1,3,5]triazines: synthesis and anticancer activity
1Velihina Ye. S., 1Pil’o S. G., 1Zyabrev V. S., 1, 2Moskvina V. S., 1, 2Shablykina O. V., 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. Synthesis of a series of 2-(dichloromethyl)pyrazolo[1,5-a][1,3,5]triazines and evaluation in vitro of their anticancer activity against a panel of 60 cell lines derived from nine cancer types, namely leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, breast cancer. Methods. Organic synthesis; biological tests; spectral methods; statistical methods. Results. In vitro screening of the anticancer activity showed that 5 of 26 tested compounds can effectively inhibit the growth of certain cancer cell lines. Conclusions. New type of N-(2,2-dichloro-1-cyanoethenyl)carboxamides heterocyclization with 1H-pyrazol-5-amines led to the formation of 2-(dichloromethyl)pyrazolo[1,5-a][1,3,5]triazines. Some of these compounds inhibit growth of certain cancer cell lines.
Keywords: in vitro screening, anticancer activity, heterocyclization, 1H-pyrazol-5-amines, pyra-zolo[1,5-a][1,3,5]triazines, 2-(dichloromethyl)pyrazolo[1,5-a][1,3,5]triazines.


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