Biopolym. Cell. 2022; 38(4):242-256.
http://dx.doi.org/10.7124/bc.000A7B
Bioorganic Chemistry
A combinatorial library of substituted 3-sulfonyl-2-imino-1,2-dihydro-5H-dipyrido[1,2-a:2’,3’-d]pyrimidin-5-ones and their anticancer activities
1Pilyo S. G., 1Demydchuk B. A., 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

Abstract

Aim. Synthesis of a combinatorial library of substituted 3-sulfonyl-2-imino-1,2-dihydro-5H-dipyrido[1,2-a:2’,3’-d]pyrimidin-5-ones and evaluation of in vitro anticancer activity against a panel of 60 different human tumor cell lines derived from nine cancer types. Methods. Organic synthesis; biological tests; spectral methods; statistic methods. Results. An efficient protocol for the synthesis of new 3-sulfonyl-2-imino-1,2-dihydro-5H-dipyrido[1,2-a:2’,3’-d]pyrimidin-5-ones has been developed. In vitro screening of the anticancer activity showed that the obtaining compounds can effectively inhibit the growth of certain cancer cell lines. Conclusions. The synthesis of a library of 3‑sulfonyl-2-imino-1,2-dihydro-5H-dipyrido[1,2-a:2’,3’-d]pyrimidin-5-ones is described. The set of compounds (25 examples) inhibits the growth of certain renal cancer lines.
Keywords: combinatorial library, heterocyclization, 1,2-dihydro-5H-dipyrido[1,2-a:2’,3’-d]pyrimidin-5-ones, pyrido[1,2-a:2’,3’-d]pyrimidinones, in vitro screening, anticancer activity
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