158326-77-3Relevant academic research and scientific papers
Inhibitors Targeting STAT5 Signaling in Myeloid Leukemias: New Tetrahydroquinoline Derivatives with Improved Antileukemic Potential
Polomski, Marion,Brachet-Botineau, Marie,Juen, Ludovic,Viaud-Massuard, Marie-Claude,Gouilleux, Fabrice,Prié, Gildas
, p. 1034 - 1046 (2021/01/25)
Signal transducers and activators of transcription 5A and 5B (STAT5A and STAT5B) are two closely related STAT family members that are crucial downstream effectors of tyrosine kinase oncoproteins such as FLT3-ITD in acute myeloid leukemia (AML) and BCR-ABL
N-aryl substituted tetrahydroquinolines having retinoid agonist, retinoid antagonist or retinoid inverse agonist type biological activity
-
, (2008/06/13)
Compounds of the formula STR1 where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist-like biological activity.
Synthesis and biological activity of 1,2,3,4-tetrahydroquinoline and 3,4-(1H)-dihydroquinolin-2-one analogs of retinoic acid
Beard, Richard L.,Teng, Min,Colon, Diana F.,Duong, Tien T.,Thacher, Scott M.,Arefieg, Taghreed,Chandraratna, Roshantha A.S.
, p. 2373 - 2378 (2007/10/03)
Retinoids are natural and synthetic analogs of the hormone retinoic acid. Retinoids are currently being investigated clinically as drugs in several areas, including dermatology and oncology. We report the synthesis and biological activity of a new series of potent, RAR-specific retinoids substituted with a 1,2,3,4-tetrahydroquinoline or a 3,4-1H)-dihydroquinolin-2-one group.
Cardioselective antiischemic ATP-sensitive potassium channel openers. 4. Structure-activity studies on benzopyranylcyanoguanidines: Replacement of the benzopyran portion
Atwal, Karnail S.,Ferrara, Francis N.,Ding, Charles Z.,Grover, Gary J.,Sleph, Paul G.,Dzwonczyk, Steven,Baird, Anne J.,Normandin, Diane E.
, p. 304 - 313 (2007/10/03)
The results of our efforts aimed at the replacement of the benzopyran ring of the lead cardiac selective antiischemic ATP-sensitive potassium channel (K(ATP)) opener (4) are described. Systematic modification of the benzopyran ring of 4 resulted in the discovery of a structurally simpler acyclic analog (8) with slightly lower antiischemic potency than the lead compound 4. Further structure-activity studies on the acyclic analog 8 provided the 2- phenoxy-3-pyridylurea analog 18 with improved antiischemic potency and selectivity compared to the benzopyran-based compound 4. These data demonstrate that the benzopyran ring of 4 and its congeners is not mandatory for antiischemic activity and cardiac selectivity. The results described in this paper also show that, as for the benzopyran class of compounds, the structure-activity relationships for the antiischemic and vasorelaxant activities of K(ATP) openers are distinct. The mechanism of action of the acyclic analogs (e.g., 18) still appears to involve K(ATP) opening as their cardioprotective effects are abolished by pretreatment with the K(ATP) blocker glyburide.
