10554-65-1Relevant articles and documents
Substituted tetrahydroisoquinolines: synthesis, characterization, antitumor activity and other biological properties
Capilla, A. Sergi,Soucek, Richard,Grau, Laura,Romero, Manel,Rubio-Martínez, Jaime,Caignard, Daniel H.,Pujol, Maria Dolors
, p. 51 - 63 (2018/01/10)
This work deals with the molecular design, synthesis and biological activity of a series of tetrahydro[1,4]dioxanisoquinolines and dimethoxyisoquinoline analogues. This study describes the synthesis strategy of these potential antitumor compounds, their multi-step synthesis and their optimization. A series of tetrahydroisoquinolines was synthesized and their cytotoxicity evaluated. Some of these tetrahydroisoquinolines showed promising KRas inhibition, antiangiogenesis activity and antiosteoporosis properties. Molecular modeling studies showed that compound 12 bind in the p1 pocket of the KRas protein making interactions with the hydrophobic residues Leu56, Tyr64, Tyr71 and Thr74 and hydrogen bonds with residues Glu37 and Asp38.
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ETA antagonists
Jae,Winn,Von Geldern,Sorensen,Chiou,Nguyen,Marsh,Opgenorth
, p. 3978 - 3984 (2007/10/03)
The synthesis and structure-activity relationships (SAR) of a series of pyrrolidine-3-carboxylic acids as endothelin antagonists are described. The data shows an increase in selectivity when the methoxy of Atrasentan (ABT-627) is replaced with methyl, and the benzodioxole is replaced with dihydrobenzofuran. Adding a fluorine further increases the binding activity and provides a metabolically stable and orally bioavailable ETA-selective antagonist.