Design, synthesis and biological evaluation of 2,5-diaryloxazolo[4,5-d]pyrimidin-7-ylamines as selective cytotoxic agents against HeLa cells
Maryna V Kachaeva, Agnieszka B Olejniczak, Marta Denel-Bobrowska, Victor V Zhirnov, Yevheniia S Velihina, Stepan G Pilyo, Volodymyr S Brovarets

TL;DR
This study designs and tests new compounds that show selective cytotoxicity against cervical cancer cells.
Contribution
The paper introduces novel 2,5-diaryloxazolo[4,5-d]pyrimidin-7-ylamine compounds with selective anticancer activity against HeLa cells.
Findings
Three compounds (1, 3, and 9) showed high cytotoxicity against HeLa cells.
Compound 9 was identified as the most promising candidate for cervical cancer treatment.
Only compounds 1, 7, and 9 demonstrated selectivity against cancer cell lines.
Abstract
Nine novel functionalized 2,5-diaryloxazolo[4,5-d]pyrimidin-7-ylamines were designed, synthesized and characterized using 1H, 13C NMR, IR spectroscopy, elemental analysis, and liquid chromatography–mass spectrometry. Their anticancer activity was assessed against human cancer cell as well as non-cancer cell lines. Three compounds, 1, 3, and 9, were the most cytotoxic to HeLa cells (IC50 = 6.13 ± 1.95, 13.99 ± 1.80 and 49.92 ± 3.98 μM, respectively). However, only compounds 1, 7, and 9 were selective against the tested lines. Compound 9 can be classified as the most attractive and promising candidate for further development against cervical adenocarcinoma.
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Taxonomy
TopicsSynthesis and biological activity · Multicomponent Synthesis of Heterocycles · Synthesis and bioactivity of alkaloids
