Biopolym. Cell. 2020; 36(1):61-74.
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.
- V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine,
1, Murmans'ka Str., Kyiv, Ukraine, 02094 - Taras Shevchenko National University of Kyiv
64, Volodymyrska Str., Kyiv, Ukraine, 01601
Abstract
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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