Synthesis and Anti‐Hypercholesterolemic Evaluations of Calcium Salts of 4‐Substituted Quinoline‐Based Mevalonic Acid

Abstract

A series of calcium (3R,5S,6E)-7-[4,6,7,8-substituted-quinoline-3-yl]-3,5-dihydroxy-hept-6-enoates was synthesized from the lactones, and the anti-hypercholesterolemic evaluation in quails was presented in this report. It was found that most of the compounds significantly decreased levels of total cholesterol and low-density lipoprotein. 2e showed better hypolipidemic effect than atorvastatin, and 2d and 2j exhibited comparable efficacy to atorvastatin. These three compounds were selected as the hypocholesterolemic candidates for further evaluation.

Facile synthesis and in vitro anticancer evaluation of a new series of tetrahydroquinoline

“…Recently, quinoline derivatives have been demonstrated to have many biological activities [ 9 , 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 , 19 ], including anticancer activity [ 20 , 21 , 22 , 23 ]. Tetrahydroquinolines ( THQs ) are important building blocks in the chemical structure of a wide range of biologically active derivatives such as pyrazolo[3,4-b] quinolines ( PQs ) and have potent anticancer activity [ 24 , 25 ].…”

Recent Progress in the Synthesis of Super-Statins

“…Similarly, more hepatoselective derivatives of rosuvastatin (e.g., derivative 9) have been investigated [28,30]. Quinoline derivatives analogous to pitavastatin (e.g., derivative 10) have also been identified as interesting targets in this context [25,32,36]. In addition, drug candidates based on other heterocyclic motifs that had previously been less frequent in statin chemistry, such as pyrazole (e.g., derivatives 11, 12, 13) [24,26,31,34] and imidazole (e.g., derivatives 14, 15) [29,33], have also been prepared and investigated within this framework (Fig.…”