- INHIBITORS OF DUAL SPECIFICITY TYROSINE PHOSPHORYLATION REGULATED KINASE 1B
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The present invention relates to compounds of formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof (I), in particular for use in the treatment, amelioration or prevention of cancer, Alzheimer, Parkinson, Down syndrome, Metabolic syndrome, Diabetes and/or osteoarthritis.
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Page/Page column 63-64
(2021/04/10)
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- Synthesis and SAR of the antistaphylococcal natural product nematophin from Xenorhabdus nematophila
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The repeated and improper use of antibiotics had led to an increased number of multiresistant bacteria. Therefore, new lead structures are needed. Here, the synthesis and an expanded structure–activity relationship of the simple and antistaphylococcal amide nematophin from Xenorhabdus nematophila and synthetic derivatives are described. Moreover, the synthesis of intrinsic fluorescent derivatives, incorporating azaindole moieties was achieved for the first time.
- Wesche, Frank,Adihou, Hélène,Wichelhaus, Thomas A.,Bode, Helge B.
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supporting information
p. 535 - 541
(2019/03/08)
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- Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors
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From four molecules, inspired by the structural features of fascaplysin, with an interesting potential to inhibit cyclin-dependent kinases (CDKs), we designed a new series of tri-heterocyclic derivatives based on 1H-pyrrolo[2,3-b]pyridine (7-azaindole) an
- Baltus, Christine B.,Jorda, Radek,Marot, Christophe,Berka, Karel,Bazgier, Václav,Kry?tof, Vladimír,Prié, Gildas,Viaud-Massuard, Marie-Claude
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p. 701 - 719
(2016/01/09)
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- Development of 3-substituted-1H-indole derivatives as NR2B/NMDA receptor antagonists
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A combined ligand-based and structure-based approach has previously allowed us to identify NR2B/NMDA receptor antagonists containing indole scaffold. In order to further explore the main structure activity relationships of this class of derivatives we herein report the design, synthesis and biological evaluation of new analogues. Some derivatives demonstrated to produce significant anticonvulsant properties and NMDA antagonism. The most active of them (3d) showed NR2B binding affinity equipotent to that of ifenprodil. These results were also corroborated by computational studies.
- Gitto, Rosaria,Luca, Laura De,Ferro, Stefania,Citraro, Rita,Sarro, Giovambattista De,Costa, Lara,Ciranna, Lucia,Chimirri, Alba
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experimental part
p. 1640 - 1647
(2009/09/08)
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- PYRIDINONYL PDK1 INHIBITORS
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The present invention provides pyridinonyl PDKl inhibitors and methods of treating cancer using the same.
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Page/Page column 84
(2008/06/13)
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- Azaindolylalkylamine derivatives as 5-hydroxytryptamine-6 ligands
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The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
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- Reactivity of 1H-Pyrrolopyridine. I. Synthesis of 3-Acetyl-7-azaindole and Related Compounds
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The bihaviour of 1H-pyrrolo(2,3-b)pyridine (7-azaindole) towards several acylating reagents are reported.The preparation of 3-acetyl-7-azaindole, 3-chloroacetyl-7-azaindole and 3-(2-hydroxyethyl)-7-azaindole are described.
- Galvez, G.,Viladoms, P.
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p. 665 - 667
(2007/10/02)
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