Design, synthesis and biological evaluation of 2,5-diaryloxazolo[4,5- <i>d</i> ]pyrimidin-7-ylamines as selective cytotoxic agents against HeLa cells
Nine novel functionalized 2,5-diaryloxazolo[4,5-<i>d</i>]pyrimidin-7-ylamines were designed, synthesized and characterized using <sup>1</sup>H, <sup>13</sup>C NMR, IR spectroscopy, elemental analysis, and liquid chromatography-mass spectrometry<i>.</i> Their anticancer activity was assessed against human cancer cell as well as non-cancer cell lines. Three compounds, <b>1</b>, <b>3</b>, and <b>9</b>, were the most cytotoxic to HeLa cells (IC<sub>50</sub> = 6.13 ± 1.95, 13.99 ± 1.80 and 49.92 ± 3.98 μM, respectively). However, only compounds <b>1</b>, <b>7</b>, and <b>9</b> were selective against the tested lines. Compound <b>9</b> can be classified as the most attractive and promising candidate for further development against cervical adenocarcinoma.
Authors
- В. С. Броварец (ORCID: https://orcid.org/0000-0001-6668-3412)
- Agnieszka B. Olejniczak (ORCID: https://orcid.org/0000-0003-4628-9017)
- Marta Denel‐Bobrowska (ORCID: https://orcid.org/0000-0003-4379-0367)
- Yevheniia Velihina (ORCID: https://orcid.org/0000-0003-1792-9919)
- Victor V Zhirnov
- Stepan G Pilyo
Institutions
- Institute of Bioorganic Chemistry and Petrochemistry V.P. Kukhar (UA)
- Institute for Medical Biology (PL)
- Institut de Chimie Organique et Analytique (FR)
- Polish Academy of Sciences (PL)
Publication Details
- Journal
- Beilstein Journal of Organic Chemistry
- Published
- 2026-03-03
- DOI
- https://doi.org/10.3762/bjoc.22.27
- Primary Topic
- Synthesis and biological activity
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Enamine