36231-81-9Relevant articles and documents
2-substituted tricyclic oxazolo[5,4-d]pyrimidine library: Design, synthesis, and cytotoxicity activity
Zeng, Yan,Nie, Lifei,Bozorov, Khurshed,Ruzi, Zukela,Song, Buer,Zhao, Jiangyu,Aisa, Haji Akber
, p. 555 - 568 (2021/11/30)
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.
Tetrahydrooxazolopyridino-oxaazaone derivative and application of tetrahydrooxazolopyridino-oxaazaone derivative
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Paragraph 0104; 0163-0167; 0206-0207, (2021/05/12)
The invention relates to a tetrahydrooxazolopyridino-oxaazaone derivative and application thereof. Specifically, the derivative tetrahydrooxazolo[5',4' : 4,5]pyridino[1, 2-a]oxaaza-11(5H)-one derivatives E1-E48. In anti-tumor activity screening, the positive control of DOX is used; the inhibition effect of the 48 tetrahydrooxazolo[5',4':4,5]pyridino[1, 2-a]oxaaza-11(5H)-one derivatives E1-E48 on Hela human cervical cancer cells, MCF-7 breast cancer cells and A549 lung cancer cells is observed, and the results show that compared with the positive control, the compounds E5, E8, E9, E20, E26, E28, E32, E34, E38, E41, E42, E44, E45, E46, E47 and E48 have the inhibition activity on the Hela cervical cancer cells, the compounds E26, E38, E42, E45, E46 and E47 have inhibitory activity on MCF-7 breast cancer cells; and the compounds E8, E9, E26 and E47 have inhibitory activity on A549 lung cancer cells.
4-SUBSTITUTED PYRIDIN-3-YL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE
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, (2011/04/18)
The invention relates to compounds of formula (I) which are useful as kinase inhibitors, more specifically useful as PIM kinase inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same, either alone or in combination, to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.