1070781-97-3Relevant academic research and scientific papers
In vitro and in vivo anti-Leishmania activity of polysubstituted synthetic chalcones
Aponte, Jose C.,Castillo, Denis,Estevez, Yannick,Gonzalez, German,Arevalo, Jorge,Hammond, Gerald B.,Sauvain, Michel
scheme or table, p. 100 - 103 (2010/04/06)
The in vitro screening of 43 polysubstituted chalcones against Leishmania amazonensis axenic amastigotes, led to the evaluation of 9 of them in a macrophage-infected model with the two other most infectious Leishmania species prevalent in Peru (L. braziliensis and L. peruviana). The five most active and selective chalcones were studied in vivo, resulting on the identification of two chalcones with high reduction parasite burden percentages.
COMPOUNDS, THEIR SYNTHESES, AND THEIR USES
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Page/Page column 43, (2010/04/03)
Embodiments of the present invention provide compounds (such as Formula (I) compounds, Formula (II) compounds, and various embodiments thereof). Compositions comprising those compounds are also provided. Methods for their preparation are included. Also, uses of the compounds are included, such as administering and treating diseases (e.g., cancer and infections).
Synthesis, cytotoxicity, and anti-Trypanosoma cruzi activity of new chalcones
Aponte, José C.,Verástegui, Manuela,Málaga, Edith,Zimic, Mirko,Quiliano, Miguel,Vaisberg, Abraham J.,Gilman, Robert H.,Hammond, Gerald B.
experimental part, p. 6230 - 6234 (2009/09/25)
Synthesis of a cytotoxic dihydrochalcone, first isolated from a traditional Amazonian medicinal plant Iryanthera juruensis Warb (Myristicaceae), followed by a comprehensive SAR analysis of saturated and unsaturated chalcone synthetic intermediates, led to the identification of analogues with selective and significant in vitro anti-Trypanosoma cruzi activity. Further SAR studies were undertaken with the synthesis of 21 new chalcones containing two allyloxy moieties that resulted in the discovery of 2′,4′-diallyloxy- 6′-methoxy chalcones with improved selectivity against this parasite at concentrations below 25 μM, four of which exhibited a selectivity index greater than 12.
