Synthesis, Anticancer Activity and Molecular Docking Studies of Some Novel Quinoline Hydrazide Derivatives of Substituted Benzaldehydes

Navigating the Synthesis of Quinoline Hybrid Molecules as Promising Anticancer Agents

“…Hybrid 128 e forms enzyme-substrate complex at the active site of tyrosine kinase through various non-covalent interactions involving Hbonding interaction of -OH and -N atom of aldehyde and quinoline moiety, implementing its active role in further design of anticancer therapeutics (Scheme 26). [91] Kanubhai D Katariya and his group prepared quinoline hydrazone analogues 131 a-p by acid-catalyzed reaction of quinoline hydrazines 129 with corresponding benzaldehyde 130. Most of quinoline hydrazone hybrids 131 b, 131 d, 131 e, 131 f, 131 g, 131 h, 131 i, 131 j, 131 l exhibited good antiproliferative activity at 10 μM concentration with GI 50 values 0.33 to 4.87 μM and LC 50 values ranging from 4.67 μM to > 100j μM.…”

Synthesis of 12-quinoline substituted andrographolide derivatives and their preliminary evaluation as anti-aggregation drugs

“…1) had better anti-platelet aggregation activity, when adenosine diphosphate (ADP) was employed as inducer. [11][12][13] Quinoline derivatives also exhibit a wide spectrum of biological activities such as anti-malarial, [14] antibacterial, [15] anti-cancer, [16] anti-oxidant, [17] anti-tuberculous, [18] anti-parasitic, [19] and anti-platelet aggregation (methyl liensinine, rhynchophylline, berberine) activities. [20][21][22] Both andrographolide and quinoline are readily available pharmacophores and have been subjects in the search for new biologically active compounds.…”

Quinoline–hydrazone hybrids as dual mutant EGFR inhibitors with promising metallic nanoparticle loading: rationalized design, synthesis, biological investigation and computational studies

“…Hybrid- I showed the most potential growth inhibitory activity with IC 50 = 1.23 μM, 1.35 μM, and 1.49 μM against LCLC-103H/large cell lung, DAN-G/pancreas, and SISO/uterine cancer cell lines, respectively. 38 Moreover, the synthesis of quinoline-hydrazides was brought to the limelight of the literature by Gayam et al 39 The cytotoxicity was studied against the K562/myelogenous leukemia cancer cell line and compound II was found to have potent activity (IC 50 = 0.06 nM) through cell proliferation assay. Katariya and his group prepared quinoline hydrazone analogues through acid-catalyzed reaction of their congruent hydrazines with the corresponding benzaldehydes.…”