2038-03-1Relevant articles and documents
SYNTHESIS, STRUCTURE, AND ACTION OF SOME GOSSYPOL DERIVATIVES ON THE PEROXIDATION OF THE LIPIDS OF BIOSUBSTRATES
Dalimov, D. N.,Mukhamedzhanova, E. N.,Shneivais, V. B.,Biktimirov, L.,Ismailov, A. I.,Kamaev, F. G.
, p. 603 - 607 (1989)
The synthesis has been effected of new gossypol derivatives using piperidino- and morpholinoethylamines.According to their PMR spectra, these substances exist in the keto-amine form.Their action on the peroxidation of lipids (POL) of various biosubstrates has been studied.Gossypol bis(piperidinoethylimine) and bis(morpholinoethylimine) in concentrations of 1*1E-7 - 5*1E-6 mM exert a pronounced antioxidant action on human blood serum and rat brain synaptosomes.In the same concentrations, these substances suppressed the POL in enzymatic and nonenzymatic systems of the oxidation of rat liver microsomes.
COMPOUND INHIBITING BUTYRYLCHOLINESTERASE
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Page/Page column 9, (2020/07/31)
The invention concerns a compound according to formula (I), wherein 3 n 11, wherein R comprises or consists of a heterocycle comprising one tertiary amino group providing the binding of R to the rest of the molecule and at least three carbon atoms, wherein all carbon atoms of the heterocycle are unsubstituted or wherein R is a fused bicyclic compound comprising the heterocycle and one further cyclic compound.
New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis
Tazarki, Helmi,Zeinyeh, Wael,Esvan, Yannick J.,Knapp, Stefan,Chatterjee, Deep,Schr?der, Martin,Joerger, Andreas C.,Khiari, Jameleddine,Josselin, Béatrice,Baratte, Blandine,Bach, Stéphane,Ruchaud, Sandrine,Anizon, Fabrice,Giraud, Francis,Moreau, Pascale
, p. 304 - 317 (2019/02/07)
Cdc2-like kinase 1 (CLK1) and dual specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) are involved in the regulation of alternative pre-mRNA splicing. Dysregulation of this process has been linked to cancer progression and neurodegenerative diseases, making CLK1 and DYRK1A important therapeutic targets. Here we describe the synthesis of new pyrido[3,4-g]quinazoline derivatives and the evaluation of the inhibitory potencies of these compounds toward CDK5, CK1, GSK3, CLK1 and DYRK1A. Introduction of aminoalkylamino groups at the 2-position resulted in several compounds with low nanomolar affinity and selective inhibition of CLK1 and/or DYRK1A. Their evaluation on several immortalized or cancerous cell lines showed varying degree of cell viability reduction. Co-crystal structures of CLK1 with two of the most potent compounds revealed two alternative binding modes of the pyrido[3,4-g]quinazoline scaffold that can be exploited for future inhibitor design.