10.1002/ardp.19853180716
The research focuses on the synthesis and cytotoxic evaluation of certain flavones against L1210 cells. The purpose of the study was to investigate the relationship between the full oxygenation of the A-ring in flavones and their cytotoxic activity, as it was observed that 5,2'-dihydroxy-6,7,8,6'-tetramethoxyflavon (6c), isolated from the root of Scutellaria baicalensis, exhibited cytotoxic activity against L1210 cells, while other flavones from the same root did not. The researchers synthesized 5,2'-dihydroxy-6,7,8,6'-tetramethoxyflavon (6c) and other flavones with the same A-ring and tested their cytotoxicity. Key chemicals used in the synthesis process included 2-benzyloxyd-methoxybenzylchlorid (2c) as the starting substance for the B-ring, and various other intermediates such as 3c, 4d, and 4c. The conclusions drawn from the study were that 5,2'-dihydroxy-6,7,8,6'-tetramethoxyflavon (6c) is the active principle of Scutellariae Radix against L1210 cells, and that two other flavones, 5d and 9, with a fully oxygenated A-ring also showed cytotoxic activity. The cytotoxic activity of the flavones was expressed as ED50 values, with 6c showing the strongest inhibition of L1210 cell growth (ED50 = 2.5 μg/ml), followed by 9 and 5d with ED50 values of 7.5 and 4.5 μg/ml, respectively.
10.1016/j.bmc.2016.04.045
The research aimed to identify and develop novel anti-HIV compounds from the class of flavonoids, specifically focusing on chalcones, coumaranones, and other flavonoid derivatives. The purpose was to screen these compounds for their anti-HIV-1 activity and to evaluate their potency and cytotoxicity in two cell culture models, TZM-bl and PM1 cells. The study concluded that O-benzyl-substituted chalcones, particularly chalcones 8o and 8p, showed promise as anti-HIV agents due to their high anti-viral potency and low cytotoxicity. These compounds significantly inhibited HIV propagation at low micromolar doses and were relatively non-toxic to the cell lines tested. The chemicals used in the process included a series of chalcone, flavone, coumaranone, and other flavonoid compounds, with specific focus on those containing an α- or β-hydroxy-carbonyl motif within their structure, such as chalcone 8l, flavonol 9c, and the newly designed chalcones 8o and 8p.
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