1522-00-5Relevant academic research and scientific papers
Design, synthesis and anticancer activity of naphthoquinone derivatives
Han, Xuan-zhen,Liu, Xinhua,Shen, Xiao-bao,Sheng, Liang-quan,Wang, Yang,Wu, Fu-fang
, p. 773 - 785 (2020/04/02)
Basis on molecular docking and pharmacophore analysis of naphthoquinone moiety, a total of 23 compounds were designed and synthesised. With the help of reverse targets searching, anti-cancer activity was preliminarily evaluated, most of them are effective against some tumour cells, especially compound 12: 1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl-4-oxo-4-((4-phenoxyphenyl)amino) butanoate whose IC50 against SGC-7901 was 4.1 ± 2.6 μM. Meanwhile the anticancer mechanism of compound 12 had been investigated by AnnexinV/PI staining, immunofluorescence, Western blot assay and molecular docking. The results indicated that this compound might induce cell apoptosis and cell autophagy through regulating the PI3K signal pathway.
Synthesis and antiischemic activity of dicarboxylic nitroxyalkylamides and nitroxyalkylimides
Fedorov,Bogdanov,Fadeev,Lagodzinskaya
, p. 1119 - 1125 (2015/04/14)
A number of dicarboxylic N-(2-nitroxyalkyl)amides and N-(2-nitroxyalkyl)imides were synthesized and their antiischemic activity was studied. The ratio of the areas of necrotic and ischemic zones was used as a criterion for evaluation of antiischemic activity. The maximum values were close to antiischemic activity of Nicorandil, with acute toxicity of compounds synthesized being considerably lower.
Synthesis and 1H NMR titration study of 7-deoxycholic amide or cholane ionophores containing different ion-recognizing groups at C3 and C12
Oh, Hyunju,Han, Sang Keun,Kim, Byeong Hyo
scheme or table, p. 187 - 194 (2012/07/13)
Tweezer-type ionophores containing C3-carbamoylpropanamidoacetoxy and C12-dithiocarbamoyl groups on a 7-deoxycholic amide or cholane derivative were designed and synthesized. A representative 1H NMR titration study indicated that newly synthesi
HETEROCYCLIC BETA-3 ADRENERGIC RECEPTOR AGONISTS
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, (2008/06/13)
This invention provides compounds of Formula I having the structure U, V, W, X, and Y are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.
Titanium tetrachloride-mediated enantioselective synthesis of trans β-lactones
Cardani, Silvia,De Toma, Carlo,Gennari, Cesare,Scolastico, Carlo
, p. 5557 - 5564 (2007/10/02)
Pharmacologically interesting trans β-lactones 11 and 16 were synthesized using a titanium tetrachloride-mediated enantioselective aldol reaction as the key synthetic step (see Scheme 2).
