<scp>2‐substituted</scp> tricyclic oxazolo[5,4‐<i>d</i>]pyrimidine library: Design, synthesis, and cytotoxicity activity
Yan ZengState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences Urumqi ChinaLifei NieState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences Urumqi ChinaKhurshed BozorovFaculty of Chemistry Samarkand State University Samarkand UzbekistanZukela RuziState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences Urumqi ChinaBuer SongState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences Urumqi ChinaJiangyu ZhaoState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences Urumqi ChinaHaji Akber AisaState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences Urumqi China
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Abstract We report the design, synthetic route, and cytotoxicity of a library of 49 newly synthesized tricyclic oxazolo[5,4‐ d ]pyrimidines. The condensed pyrimidinones were constructed from ethyl 5‐aminooxazole‐4‐carboxylate building blocks. A tricyclic ring system was built using the naturally occurring mackinazolinone alkaloid with a focus on the molecular diversity at position C‐2 of the oxazole ring. Synthesized compounds were evaluated against a panel of human cancer cell lines including MCF‐7 (breast), HeLa (cervical), and A549 (lung) in vitro. The results revealed that substitution of halogen‐related aromatic fragments at position C‐2 of the oxazole ring may serve as promising anticancer drug candidates.
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