European Journal of Medicinal Chemistry p. 51 - 63 (2018)
Update date:2022-08-04
Topics: Characterization Antimicrobial activity Structure-Activity Relationship (SAR) Drug Development Antioxidant Activity Anti-Inflammatory Activity Synthesis of Substituted Tetrahydroisoquinolines Substituted THIQs have shown promising antitumor activities in various preclinical and clinical studies. They can exhibit their antitumor effects through multiple mechanisms, such as Neuroprotective Activity
Capilla, A. Sergi
Soucek, Richard
Grau, Laura
Romero, Manel
Rubio-Martínez, Jaime
Caignard, Daniel H.
Pujol, Maria Dolors
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.
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