949580-77-2Relevant academic research and scientific papers
Synthesis and biological evaluation of resveratrol-coumarin hybrid compounds as potential antitumor agents
Shen, Wei,Mao, Jianfeng,Sun, Juan,Sun, Minjie,Zhang, Can
, p. 1630 - 1640 (2013/07/26)
Eighteen resveratrol-coumarin hybrid compounds (6 or 7-styryl-3- phenylcoumarin) were designed, synthesized and thirteen compounds were evaluated for their antitumor activities against MCF-7, HCT-28, and K562 tumor cell lines. Among them, compounds 2Z, 2E, 5E, and 7E showed varying degrees of growth inhibition of the above cell lines (IC50: 3.78-19.16 μmol/L). On the basis of the biological results, structure-activity relationships were obtained and discussed.
Extensive SAR and computational studies of 3-{4-[(benzylmethylamino)methyl] phenyl}-6,7-dimethoxy-2H-2-chromenone (AP2238) derivatives
Piazzi, Lorna,Cavalli, Andrea,Belluti, Federica,Bisi, Alessandra,Gobbi, Silvia,Rizzo, Stefano,Bartolini, Manuela,Andrisano, Vincenza,Recanatini, Maurizio,Rampa, Angela
, p. 4250 - 4254 (2008/02/11)
AP2238 was the first compound published to bind both anionic sites of the human acetylcholinesterase, allowing the simultaneous inhibition of the catalytic and the amyloid-β pro-aggregating activities of AChE. Here we attempted to derive a comprehensive structure-activity relationship picture for this molecule, affording 28 derivatives for which AChE and BChE inhibitory activities were evaluated. Selected compounds were also tested for their ability to prevent the AChE-induced Aβ-aggregation. Moreover, docking simulations and molecular orbital calculations were performed.
