Effect of side chain location in (2-aminoethyl)aminomethyl-2-phenylquinolines as antitumor agents

Curcumin and cyclopalladated complexes: A recipe for bifunctional biomaterials

“…Of the several organic ligands capable of cyclometallation, 2-phenylquinoline and its 4-substituted derivatives, are an important class of bioactive ligands whose properties, ranging from antibacterial [3] antiplatelet [4], antihypertensive [5], antitumor [6,7], are mainly ascribed to their DNA or RNA intercalation binding. Despite the extensive literature concerning the photophysical and electrochemical properties of cyclometallated iridium(III) and platinum(II) complexes [8,9] based on a 2-phenylquinoline framework, no 2-phenylquinoline metallacycle derivatives have been studied for their therapeutic properties.…”

Synthesis and evaluation of antibacterial and antioxidant activity of novel 2-phenyl-quinoline analogs derivatized at position 4 with aromatically substituted 4H-1,2,4-triazoles

“…On the other hand, quinoline derivatives are known to possess diverse pharmacological properties such as antioxidant 18,19 , antibiotic 20,21 , cardiovascular 22 , anti-TB 23 , antiplatelet 24 , anticancer 25,26 , receptor antagonists 27 , NK3 receptor antagonists-II 28 , anti-inflammatory 29 , antimicrobial 30,31 , selective estrogen receptor modulators (SERMs) 32 and protein kinase inhibitor 33 . Keeping above in mind, we decided to synthesize conjugates of the above-mentioned moieties to study the biological profile of the resulting product.…”

Synthesis, Antiproliferative Evaluation, and Structure–Activity Relationships of 3‐Arylquinolines

“…[7] More over, some aza analogues of the 2-phenyl-naphthalenes (1), 2-phenylquinolines (4), possessed interesting biological activities. [15,16] However, the 3-phenylquinoline (5) derivatives have yet to be investigated as potential anticancer agents. While no antitumor activity has been reported for the 3-phenylquinolines (5), the similarity in biological activities between the 2-phenyl-4-quinolones (2) and 3-phenyl-4-quinolones (3), [17,18] suggests that the 3-phenylquinolines (5) should exhibit similar biological activities to the 2-phenylquinolines (4), and be of interest as new chemotherapeutics.…”

“…[19] The 3-phenylquinolines are expected to act through the same mechanism of action as the 2-phenylquinolines, which are known to intercalate DNA leading to inhibition of mammalian topoisomerase II. [15,16,20] In order to identify potent potential lead compounds, and probe the structure-activity relationships (SAR) within these compounds, both the phenyl and quinoline ring were substituted with groups of varying steric, electronic, and lipophilic properties.…”