- Novel vitexin-inspired scaffold against leukemia
-
Acute lymphoblastic leukemia (ALL) is the most common type of leukemia in children. Up to a quarter of ALL patients relapse and face poor prognosis. To identify new compound leads, we conducted a phenotypic screen using terrestrial natural product (NP) fr
- Ling, Taotao,Lang, Walter,Feng, Xiang,Das, Sourav,Maier, Julie,Jeffries, Cynthia,Shelat, Anang,Rivas, Fatima
-
supporting information
p. 501 - 510
(2018/02/15)
-
- Kynurenic acid amides as novel NR2B selective NMDA receptor antagonists
-
A novel series of kynurenic acid amides, ring-enlarged derivatives of indole-2-carboxamides, was prepared and identified as in vivo active NR2B subtype selective NMDA receptor antagonists. The synthesis and SAR studies are discussed.
- Borza, Istvan,Kolok, Sandor,Galgoczy, Kornel,Gere, Aniko,Horvath, Csilla,Farkas, Sandor,Greiner, Istvan,Domany, Gyoergy
-
p. 406 - 409
(2007/10/03)
-
- 2-AMINOCARBONYL-QUINOLINE COMPOUNDS AS PLATELET ADENOSINE DIPHOSPHATE RECEPTOR ANTAGONISTS
-
Compounds of formula (I), where m, n, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.
- -
-
-
- Platelet adenosine diphosphate receptor antagonists
-
Compounds of the following formula (I): where a, b, R1, R2, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, met
- -
-
-
- Amide derivatives and nociceptin antagonists
-
The present invention relates to a compound of the formula [1′] wherein R2is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R5is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R5may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1′] as an active ingredient. The compound [1′] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1′] as a nociceptin antagonist or analgesic.
- -
-
-
- Kynurenic acid derivatives inhibit the binding of nerve growth factor (NGF) to the low-affinity p75 NGF receptor
-
The ability of a series of substituted kynurenic acids, thienopyridinonecarboxylic acids, and related compounds to inhibit the binding of nerve growth factor (NGF) to the p75 NGF receptor (NGFR) was evaluated in a radioligand binding assay that utilized a
- Jaen,Laborde,Bucsh,Caprathe,Sorenson,Fergus,Spiegel,Marks,Dickerson,Davis
-
p. 4439 - 4445
(2007/10/03)
-