Informace o publikaci
BIOLOGICALLY ACTIVE DIHYDROPYRROLO[1,2-b]PYRAZOLE DERIVATIVES AND THEIR SYNTHESES
| Autoři | |
|---|---|
| Rok publikování | 2015 |
| Druh | Článek ve sborníku |
| Konference | Bioheterocycles 2015 - XVI International Conference on Heterocycles in Bioorganic Chemistry , Book of Abstracts |
| Fakulta / Pracoviště MU | |
| Citace | |
| Obor | Organická chemie |
| Popis | Variously substituted dihydropyrrolo[1,2-b]pyrazoles are characterized by interesting biological properties. Their biological activity is described by controlling cytokinins in processes connected with growth and differentiation of cells.1-2 In our laboratory in the synthesis of the basic skeleton we concentrated upon application of substituted homoallenyl aldehyde, which properties were already examined. We found that prepared non-symmetrical allenyl alkyl azine when heated in boiling xylene afforded corresponding dihydropyrrolo[1,2-b]pyrazole skeleton 3. This way obtained basic skeleton was in following reactions modified. A number of new skeletons shown at Scheme was due to the structural similarity with ALK5 inhibitor LY2109761, subjected in vitro testing to their anticancer activity against human cancer cell lines and inhibition of protein kinases ALK5, ABL and CDK2. Besides, computer docking for biological property improvement of synthesized compounds was carried out. |