Synthesis, Characterization, and In vitro Anticancer Evaluation of 7-Piperazin-Substituted [1,3]Oxazolo[4,5-D]Pyrimidines

Yevgeniya S Velihina; Maryna V Kachaeva; Stepan G Pilyo; Victor V Zhirnov; Volodymyr S Brovarets

Abstract

Synthesis, Characterization, and In vitro Anticancer Evaluation of 7-Piperazin-Substituted [1,3]Oxazolo[4,5-D]Pyrimidines

Author(s): Yevgeniya S Velihina, Maryna V Kachaeva, Stepan G Pilyo, Victor V Zhirnov, Volodymyr S Brovarets

A novel series of five 7-piperazin-substituted [1,3]oxazolo[4,5-d]pyrimidines have been synthesized and characterized by Infrared (IR), Proton Nuclear Magnetic Resonance (¹H-NMR), Carbon-13 Nuclear Magnetic Resonance (¹³C-NMR) spectroscopy, elemental analysis and chromato-mass-spectrometry. The anticancer activities of the all the newly synthesized compounds were valuated via single high dose (10^-5M) against 60 cancer cell lines by the National Cancer Institute according to its own screening protocol. In the next phase, the compounds have been selected for five-dose assay. Among these compounds 5-phenyl-7-piperazin-1-yl-2-p-tolyl[1,3]oxazolo[4,5-d]pyrimidine displayed the most growth inhibitory (GI₅₀ was in range of 0.2−2.0 μM), cytostatic (TGI − 0.3-4.2 μM) and cytotoxic (LC₅₀ − 0.6-7.8 μM with the exception of Leukemia CCRF-CEM cell line, LC₅₀>100 μM) activities against all cancer cell lines. The most selectivity 5-phenyl-7-piperazin-1-yl-2-p-tolyl[1,3]oxazolo[4,5-d]pyrimidine demonstrated against Leukemia and Colon Cancer subpanels. These results provided evidence that compound could be useful for developing new anticancer drugs.

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