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result sql = Total synthesis, antiprotozoal and cytotoxicity activities of rhuschalcone VI and analogs.
Total synthesis, antiprotozoal and cytotoxicity activities of rhuschalcone VI and analogs.
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result sql = The total synthesis of a potent antiplasmodial natural bichalcone, rhuschalcone VI, is described starting from simple and available resorcinol and 4-hydroxybenzaldehyde. Key steps include the solvent-free Aldol syntheses of chalcones, and the successful application of the Suzuki-Miyaura coupling reaction in the synthesis of bichalcones. The present work constitutes a general method for the rapid syntheses of a number of bichalcones related to rhuschalcone VI. Some of the bichalcones showed moderate antiprotozoal activities against Bodo caudatus, a preliminary screening system for antitrypanosomal activities, most of them with little or no cytotoxicity.

Publication: Bioorg. Med. Chem. 2010 Apr 1 ;18(7)::2464-73. :doi: 10.1016/j.bmc.2010.02.055.
Publication Date: 2010 Apr 1
Study Author(s): Mihigo, Shetonde O;Mammo, Wendimagegn;Bezabih, Merhatibeb;Andrae-Marobela, Kerstin;Abegaz, Berhanu M;
Institution: Department of Chemistry, University of Botswana, P. Bag 00704, Gaborone, Botswana.
Shortcut link to this study:
The total synthesis of a potent antiplasmodial natural bichalcone, rhuschalcone VI, is described starting from simple and available resorcinol and 4-hydroxybenzaldehyde. Key steps include the solvent-free Aldol syntheses of chalcones, and the successful application of the Suzuki-Miyaura coupling reaction in the synthesis of bichalcones. The present work constitutes a general method for the rapid syntheses of a number of bichalcones related to rhuschalcone VI. Some of the bichalcones showed moderate antiprotozoal activities against Bodo caudatus, a preliminary screening system for antitrypanosomal activities, most of them with little or no cytotoxicity.
PMID: 20304658

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