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Synthesis and anti-proliferative activity of a small library of 7-substituted 5H-pyrrole [1,2-a][3,1]benzoxazin-5-one derivatives.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Jul2017, Vol. 27 Issue 14, p3092-3095. 4p. - Publication Year :
- 2017
-
Abstract
- In this study, we investigate the anti-proliferative activity of a small library of 7-substituted 5 H -pyrrolo[1,2- a ][3,1]benzoxazin-5-one derivatives, against a panel of human cancer cell lines. We reported the synthesis of these compounds in a previous work. 7-Bromo-5 H -benzo[ d ]pyrrolo[2,1- b ][1,3]oxazin-5-one showed a promising anti-proliferative effect. As starting material for Suzuki-Miyaura cross coupling reaction, it was selected for the design and the synthesis of six further derivatives, with the aim to better define structure-activity relationships. The anti-proliferative MTT assay revealed a dose-dependent reduction of cell viability, especially for 7-([1,1′-biphenyl]-4-yl)-5 H -benzo[ d ]pyrrolo[2,1- b ][1,3]oxazin-5-one. Cell cycle and western blotting analysis suggested apoptosis as possible mechanism for its anti-proliferative activity. These preliminary results encourage our interest for further optimizations. [ABSTRACT FROM AUTHOR]
- Subjects :
- *PYRROLES
*BENZOXAZINES
*CHEMICAL derivatives
*APOPTOSIS
*CELL death
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 27
- Issue :
- 14
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 123504516
- Full Text :
- https://doi.org/10.1016/j.bmcl.2017.05.046