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5-Oxo-hexahydroquinoline and 5-oxo-tetrahydrocyclopentapyridine derivatives as promising antiproliferative agents with p...

Published in Molecular diversity

Discovery of novel anticancer agents is of crucial importance to expand the therapeutic options for cancer patients. In this study, a series of 49 5-oxo-hexahydroquinoline and 5-oxo-tetrahydrocyclopentapyridine analogs, containing different pyridine alkyl carboxylates at C3 and various aliphatic, aromatic, and heteroaromatic substitutions at the C4...

Synthesis and Antimalarial Activities of New Hybrid Atokel Molecules

Published in ChemistryOpen

Novel Atokel molecules were designed as putative antimalarial drugs combining, in a single molecule, the naphthoquinone residue of atovaquone, an antimalarial drug targeting the parasite mitochondrion, and a copper chelator expected to induce, in presence of biologically available copper ions, a lethal oxidative stress.

Spectroscopic analysis of 2-(5-mercapto-1,3,4-oxadiazol-2-yl)-6-methylquinolin-4-ol binding to blood plasma albumin

Published in Monatshefte Fur Chemie

Binding of 2-(5-mercapto-1,3,4-oxadiazol-2-yl)-6-methylquinolin-4-ol (C1), a biologically active substance, to bovine blood plasma albumin (BSA) at 293, 298, and 303 K was studied using fluorescence (steady state, synchronous, excitation/emission matrix) and FT-IR spectroscopy methods. The experimental results showed that C1 causes fluorescence que...

Anthranilamides with quinoline and β-carboline scaffolds: design, synthesis, and biological activity

Published in Molecular Diversity

In the present study, we report the design and synthesis of novel amide-type hybrid molecules based on anthranilic acid and quinoline or β-carboline heterocyclic scaffolds. Three types of biological screenings were performed: (i) in vitro antiproliferative screening against a panel of solid tumor and leukemia cell lines, (ii) antiviral screening ag...

2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluat...

Published in Journal of Enzyme Inhibition and Medicinal Chemistry

Synthesis and potential antimicrobial activity of novel α-aminophosphonates derivatives bearing substituted quinoline or...

Published in Medicinal Chemistry Research

To develop novel antimicrobial agents, and based on the biologically active heterocyclic quinoline and thiazole substituted, a series of novel α-aminophosphonates ( 9a – h ) and ( 10i – l ) derivatives that incorporated quinoline or quinolone, and coumarylthiazole or 5-phenylthiazol-2-amine moieties were designed and synthesized via Kabachnik–Field...

Synthesis, antimicrobial evaluation, and in silico studies of quinoline-1H-1,2,3-triazole molecular hybrids.

Published in Molecular diversity

Antimicrobial resistance has become a significant threat to global public health, thus precipitating an exigent need for new drugs with improved therapeutic efficacy. In this regard, molecular hybridization is deemed as a viable strategy to afford multi-target-based drug candidates. Herein, we report a library of quinoline-1H-1,2,3-triazole molecul...

Antifungal activity of nitroxoline against Candida auris isolates.

Published in Clinical microbiology and infection : the official publication of the European Society of Clinical Microbiology and Infectious Diseases

To investigate the in vitro activity of nitroxoline against a molecularly characterized collection of clinical Candida auris isolates. Thirty-five clinical isolates of C. auris from diverse sources representing all five different C. auris clades were included in the study. Nitroxoline activity was assessed using broth microdilution. Additionally, s...

Synthesis, antitubercular, antimicrobial activities and molecular docking study of quinoline bearing dihydropyrimidines....

Published in Bioorganic chemistry

In order to develop the antimicrobial and antitubercular agents, we have derived quinoline bearing dihydropyrimidine analogues 5a-o and structures of these compounds were determined by spectroscopic techniques. Further, we have calculated the molecular properties prediction and drug-likeness by Molinspiration property calculation toolkit and MolSof...

Free energy perturbation guided Synthesis with Biological Evaluation of Substituted Quinoline derivatives as small molec...

Published in Bioorganic chemistry

Two different schemes of novel substituted quinoline derivatives were designed and synthesized via simple reaction steps and conditions. A comparative molecular docking study was carried out on two different types of EGFR enzymes which include wild-type (PDB: 4I23) and T790M mutated (PDB: 2JIV) respectively. Compounds were also validated upon T790M...