52146-70-0Relevant academic research and scientific papers
Inhibition of reverse transcriptase and Taq DNA polymerase by compounds possessing the coumarin framework
Garro Hugo,Manzur Jimena,Ciuffo Gladys,Tonn Carlos,Pungitore Carlos
, p. 760 - 764 (2014/02/14)
Coumarin derivatives were prepared using natural products isolated from plants belonging in the Pterocaulon genus (Asteraceae) and commercial drugs. Some molecules have displayed interesting activity against myeloid murine leukemia virus-reverse transcriptase (MMLV-RT) (compounds 20 and 28 produced inhibition with IC50 values of 38.62 and 50.98 μM, respectively) and Taq DNA polymerase (analogues 13 and 14 produced inhibition with IC 50 values of 48.08 and 57.88 μM, respectively). Such inhibitors may have importance as antiretroviral chemotherapeutic agents and also in the development of anticancer drugs.
Toward establishing structure-activity relationships for oxygenated coumarins as differentiation inducers of promonocytic leukemic cells
Riveiro, Maria E.,Maes, Dominick,Vazquez, Ramiro,Vermeulen, Monica,Mangelinckx, Sven,Jacobs, Jan,Debenedetti, Silvia,Shayo, Carina,De Kimpe, Norbert,Davio, Carlos
experimental part, p. 6547 - 6559 (2009/12/09)
The presumption that some coumarins might be lead compounds in the search for new differentiation agents against leukemia is based on the fact that natural coumarins, 5-(3-methyl-2-butenyloxy)-6,7-methylenedioxycoumarin (C-2) and 5-methoxy-6,7-methylenedioxycoumarin (C-1) inhibit proliferation and induce differentiation in U-937 cells [Riveiro, M. E.; Shayo, C.; Monczor, F.; Fernandez, N.; Baldi, A.; De Kimpe, N.; Rossi, J.; Debenedetti, S.; Davio, C. Cancer Lett. 2004, 210, 179-188]. These promising findings prompted us to investigate the anti-leukemia activity of a broader range of related polyoxygenated coumarins. Twenty related natural or synthetically prepared coumarins, including a range of 5-substituted ayapin derivatives which have become easy accessible via newly developed synthesis methods, were evaluated, where treatments with 5-(2,3-dihydroxy-3-methylbutoxy)-6,7-methylenedioxycoumarin (D-3) and 5-(2-hydroxy-3-methoxy-3-methylbutoxy)-6,7-methylenedioxycoumarin (D-2) were able to inhibit the cell growth and induce the differentiation of U-937 cells after 48 h treatment. These results provide insight into the correlation between some structural properties of polyoxygenated coumarins and their in vitro leukemic differentiation activity.
