Синтез та протиракова активність 2,5-діарил-оксазоло[5,4-d]піримідин-7-амінів та відповідних амідів

• Date: 2025
• Main Authors: Pilyo, Stepan G., Kachaeva, Maryna V., Popilnichenko, Serhii V., Brovarets, Volodymyr S.
• Format: Article
• Language: English
• Published: V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine 2025
• Subjects: оксазоло[5,4-d]піримідин-7-амін; аміди; протипухлинна активність
• Online Access: https://bioorganica.com.ua/index.php/journal/article/view/127
• Journal Title: Ukrainica Bioorganica Acta

A series of novel oxazolo[5,4-d]pyrimidine derivatives were synthesized and evaluated for anticancer activity against NCI 60 cancer cell lines. This work is a continuation of our investigation of the anticancer activity of a number of isomeric oxazolopyrimidines, and the study of the dependence of structure on anticancer effect. Previously described oxazolo[4,5-d]pyrimidines containing N-unsubstituted amino groups of piperazine or diazepane exhibited high cytotoxicity, with submicromolar IC₅₀ values against breast (MDA-MB-231), ovarian (OVCAR-3), and colon (HCT-116) cancer cell lines in NCI screening. Synthesized 2,5-diaryl-oxazolo[5,4-d]pyrimidin-7-amines did not demonstrate significant anticancer effects, unlike the previously described isomeric oxazolo[4,5-d]pyrimidines. Inhibition activity was observed for 7-amino-2-phenyl-5-(4-methylphenyl)oxazolo[5,4-d]pyrimidine (D-765554), particularly against the MCF7 (79.6%), UO-31 (78.4%), and OVCAR-5 (88.1%) cell lines, but anticancer potential among the tested oxazolo[5,4-d]pyrimidine derivatives was not noticeable. The results of anticancer activity in the oxazolopyrimidine series, obtained in this work and published previously, may be useful for studying the bioactivity of oxazolopyrimidines in the future