881909-51-9Relevant academic research and scientific papers
Synthesis and antiproliferative evaluation of glucosylated pyrazole analogs of K252c
Douara, Bachir,Esvan, Yannick J.,Pereira, Elisabeth,Giraud, Francis,Volodina, Yulia L.,Kaluzhny, Dmitry N.,Shtil, Alexander A.,Anizon, Fabrice,Moreau, Pascale
, p. 892 - 901 (2018/01/27)
Pyrazole analogs of the staurosporine aglycon K252c were recently described as potent inhibitors of the three Pim protein kinase isoforms. To evaluate the impact of the introduction of a sugar moiety on the biological activities of this heterocyclic scaffold, four new glucosylated pyrazole analogs of K252c were synthesized. Their biological evaluation demonstrated that most active compounds 11 and 19 substituted by a β-D-glucosyl moiety at N12 or N13 positions exhibited antiproliferative activities toward HCT116 cells.
1-( -D-GLYCOPYRANOSYL)-3-SUBSTITUTED NITROGENOUS HETEROCYCLIC COMPOUND, MEDICINAL COMPOSITION CONTAINING THE SAME, AND MEDICINAL USE THEREOF
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Page/Page column 16-17, (2010/11/27)
A compound having SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity, etc. It is a 1-(β-D-glycopyranosyl)-3-substituted nitrogen-containing heterocyclic compound represented by the general formula (I), a prodrug, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof; an SGLT inhibitor containing the same; a pharmaceutical composition containing the same and a medicinal use thereof. In the formula, ring A represents optionally substituted aryl or heteroaryl; Q1 to Q5 independently represent a carbon atom having a hydrogen atom or substituent bonded thereto or a nitrogen atom; E represents a single bond, alkylene, -O-, -S- or -NH-; and R.represents methyl, ethyl, fluoromethyl or hydroxymethyl.
